Pharmacology Flashcards
(149 cards)
1
Q
Drugs causing Myalgia
A
Cimetidine
Cocaine, Heroin, Methadone
Cyclosporine
Danazol
Emetine
Epsilon aminocaproic acid
Statins
Gold
Labetolol
D-penicillamine
L-Tryptophan
Zidovudine
2
Q
Drug causing Myopathies
A
Vecuronium, Suxamethanium, Rocuronium = Neuromuscular blockers
Statins, Fibrates, Niacin (anti Lipids)
Glucocorticoids - chronic proximal myopathy or acute quadriparesis
D penicillamine: Autoimmune, Polymyositis, MG,
Chloroquin, Hydroxy-chloroquin
Amiodarone (amphophillic cationic drugs)
Colchicine (anti-microtubule)
3
Q
Topiramate Birth Defects
A
Topamax (topiramate) is an anticonvulsant drug used for the treatment of epilepsy, migraine headaches, sleeping and eating disorders, and for weight loss.
Persistent Pulmonary Hypertension of the Newborn (PPHN)
Various heart defects
Neural tube defects
Spina Bifida
Limb malformations
Lung defects
4
Q
Ondansetron in First Trimester
A
Approximately 80 percent of women suffer from nausea and vomiting during pregnancy, and about one million take Zofran or its generic version every year. A study published in the December 2014 issue of the American Journal of Obstetrics and Gynecology discussed the risks taken by pregnant women who use Zofran. The study found a two-fold increased risk of cardiac malfunction associated with Zofran, leading to an overall 30 percent increased risk of major congenital malformations.
5
Q
Codeine in Pregnancy
A
Links have been found between the use of codeine during the first trimester and the incidence of certain congenital heart defects, along with spina bifida, hydrocephaly, glaucoma, and gastroschisis.
6
Q
Teratogenic Drugs, common
A
Teratogenic drugs and birth defects
Each of the following drugs or drug groups may cause birth defects in a developing fetus:
ACE (angiotensin converting enzyme) inhibitors
angiotensin II antagonist
isotretinoin (an acne drug)
alcohol
cocaine
high doses of vitamin A
lithium
male hormones
some antibiotics
some anticonvulsant medications
some cancer-fighting medications
some drugs that treat certain rheumatic conditions
some thyroid medications
thalidomide
the blood-thinning drug warfarin
the hormone diethylstilbestrol (DES).
7
Q
Pregnancy Risk Classification of drugs
A
The classifications include:
A – Drugs that have been taken by a large number of pregnant women without any proven increase risk of birth defect.
B – Drugs that have been taken by only a limited number of pregnant women. Human data is lacking and they are further categorised based on available data from animal studies.
B1 – animal studies have not shown any increased risk.
B2 – animal studies are limited, but there does not seem to be any increased risk.
B3 – animal studies show an increased risk, but it is not clear if this risk applies to humans.
C – Drugs that, due to their effects, may cause harm to the fetus without causing birth defects. These effects may be reversible.
D – Drugs that have caused or may cause birth defects; however, the health benefit may outweigh the risk.
X – Drugs that have a high risk of birth defects and should not be used during pregnancy.
8
Q
Warfarin
A
= Vitamin K blocker, increases INR by blocking fat soluble Vitamin K dependent clotting factors as 2, 7,9,10 synthesis
= Dose, 0.5 mg to 1/2/3/4/5 etc OD
= Cheap, needs monthly INR monitoring
= Food - drug can lower or increase effects
= Antidote in case of bleeding: Vitamin Oral/IM or IV
= Prothrombin complex concentrate in case of life threatening bleeding
= INR > 5 but no bleeding: Just stop for few days, re check INR and re start lower dose
= Always tell GP, Pharmacist if starting new medications in future
= Sit with dietician to understand what food interacts with Warfarin, increase its effect and puts you at risk
= Diarrhea, vomiting. can alter effects so watch
9
Q
Rivaroxaban
Endoxaban
Apixaban
Dabigatran
A
Rivaroxaban, 15-20 mg OD
Endoxaban 30-60 mg OD
Apixaban 2.5-5 mg BD
= Factor Xa inhibitors
= Antidote: Adexanate alfa (Andexxa) - recombinant modified Factor Xa protein approved by the FDA in May 2018 to reverse apixaban and rivaroxaban in patients with life-threatening or uncontrolled bleeding. Start the bolus at a target rate of approximately 30 mg/min. Within two minutes following the bolus dose, administer the continuous IV infusion for up to 120 minutes.
Dabigatran: 110-150 mg BiD, anti-IIa
Antidote: a monoclonal antibody used as a reversal agent for dabigatran. binds to dabigatran and its acyl glucuronide metabolites with higher affinity than the binding affinity of dabigatran to thrombin, neutralizing their anticoagulant effect immediately after administration. The recommended dose is 5 g idarucizumab (2 vials of 2.5 g/50 mL)
Monitoring: direct thrombin time
10
Q
Dotrecogin alfa, Xigris
A
Drotrecogin alfa is a recombinant form of human activated protein C that has anti-thrombotic, anti-inflammatory, and profibrinolytic properties. Drotrecogin alpha belongs to the class of serine proteases. Drotrecogin alfa has not been found to improve outcomes in people with severe sepsis.
Xigris should be administered intravenously at an infusion rate of 24 mcg/kg/hr (based on actual body weight) for a total duration of infusion of 96 hours. Cost - 6800 $ per course of 96 Hrs.
Has been withdrawn from market.
11
Q
Infliximab, Remicade
A
Infliximab, a chimeric monoclonal antibody, sold under the brand name Remicade among others, is a medication used to treat a number of autoimmune diseases. This includes Crohn’s disease, ulcerative colitis, rheumatoid arthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, and Behçet’s disease.
The recommended dosage of REMICADE® is 5 mg/kg given as an intravenous induction regimen at 0, 2, and 6 weeks, followed by a maintenance regimen of 5 mg/kg every 8 weeks thereafter for the treatment of active PsA.
Remicade belongs to a drug class called tumor necrosis factor-alpha (TNF-alpha) blockers.
Can activate TB.
12
Q
C1 esterase Inhibitors
Berinert/Haegarda/ Cinryze
A
= Used in deficiency of them which leads to Hereditary angioedema which doesnot respond to Epinephrine. Most episodes or attacks are difficult to predict, and triggers vary from person to person. These triggers may include anxiety, surgery, dental procedures, medications and illnesses such as colds and flu.
= Human C1-esterase inhibitor concentrate (C1-INH concentrate) is derived from human plasma. Cinryze and Haegarda are indicated for routine prophylaxis in adults and adolescents. Berinert and Cinryze are administered as an intravenous infusion, whereas Haegarda is administered as a subcutaneous injection.
= C1 inhibitor is an acute phase reactant and a serine protease inhibitor (serpin). Serpins inhibit the steps in the lectin complement pathway as well as kinin-producing pathways. While C1 inhibitor has many functions, its function in the kinin pathway leads to angioedema.
= BERINERT is used in adults and children to treat swelling and/or painful attacks of hereditary angioedema (HAE) affecting the abdomen, face or throat. The safety and efficacy of BERINERT in preventing HAE attacks have not been established.
13
Q
Tacrolimus
A
= a calcineurin-inhibitor.
= IV Dose of Prograf injection is 0.03-0.05 mg/kg/day in kidney and liver transplant and 0.01 mg/kg/day in heart transplant given as a continuous IV infusion.
= Common SE: Hyperglycemia, Infections, Nephrotoxicity, Hyperkalemia, Reversible Encephalopathy syndrome, Liver toxic etc
= Risk of NHL and skin cancers
= metabolised by the cytochrome P450 system of liver enzymes
In T-cells, activation of the T-cell receptor normally increases intracellular calcium, which acts via calmodulin to activate calcineurin. Calcineurin then dephosphorylates the transcription factor nuclear factor of activated T-cells (NF-AT), which moves to the nucleus of the T-cell and increases the activity of genes coding for IL-2 and related cytokines. Tacrolimus prevents the dephosphorylation of NF-AT.
14
Q
Liver Enzyme Inhibitors
A
Macrolide antibiotics including erythromycin and clarithromycin, as well as several of the newer classes of antifungals, especially of the azole class (fluconazole, voriconazole), increase tacrolimus levels by competing for cytochrome enzymes.
15
Q
Ciclosporin
A
a type of drug known as a disease-modifying anti-rheumatic drug, or DMARD.
a calcineurin inhibitor,
It slows down your immune system to prevent your body from rejecting a transplanted organ. This medication can also treat rheumatoid arthritis and psoriasis. isolated in 1971 from the fungus Tolypocladium inflatum.
SE: Gum hypertrophy, convulsions, Peptic ulcers, Hirsutism, Pancreatitis, High BP, High Lipids, Infections, Neuropathies, etc
Uses: Rheumatoid diseases, Transplants, GVHD, Psoriasis, Kerato-conjunctivitis sicca,
Can leads to Squamose cell Skin Cancers and NHL
16
Q
Rituximab, anti CD 20
A
Rituximab is a chimeric monoclonal antibody against CD20 which is a surface antigen present on B cells. Therefore, it acts by depleting normal as well as pathogenic B cells while sparing plasma cells and hematopoietic stem cells as they do not express the CD20 surface antigen.
Rituximab is indicated to treat:
= non-Hodgkin lymphoma (NHL)
= chronic lymphocytic leukemia (CLL)
= rheumatoid having inadequate response to one or more TNF inhibitors
= vasculitis as granulomatosis with polyangiitis and microscopic polyangiitis
= moderate to severe pemphigus vulgaris
= combination with chemo for children (≥6 months to <18 years) with previously untreated, advanced stage, CD20-positive diffuse large B-cell lymphoma (DLBCL), Burkitt lymphoma (BL), Burkitt-like lymphoma (BLL), or mature B-cell acute leukemia (B-AL).
Common SE: often occur within two hours of the medication given include rash, itchiness, low blood pressure, and shortness of breath. Infections are also common.
Severe SE: include reactivation of hepatitis B in those previously infected, progressive multifocal leukoencephalopathy, toxic epidermal necrolysis, and death. It is unclear if use during pregnancy is safe for the developing fetus or newborn baby, but it is not proven harmful.
17
Q
Biphosphonates
Alendronate
Palmdronate
Zoledronate
Etidronate
Clodronate
A
Bisphosphonates inhibit the digestion of bone by encouraging osteoclasts to undergo apoptosis, or cell death, thereby slowing bone loss.
= Prevention and treatment of osteoporosis,
= Paget’s disease of bone, bone metastasis (with or without hypercalcemia),
= Multiple myeloma,
= Primary hyperparathyroidism,
= Osteogenesis imperfecta,
= Fibrous dysplasia, and other conditions that exhibit bone fragility.
common SE: Esophagitis, Gastritis, Flu like symptoms
Long Term SE: bisphosphonate fractures”) in the femur (thigh bone) in the shaft (diaphysis or sub-trochanteric region) of the bone, rather than at the femoral neck, which is the most common site of fracture.
18
Q
Non Biphosphonate options
A
Strontium: = The use of strontium ranelate (strontium salt of Ranelic acid) is restricted because of increased risk of venous thromboembolism, pulmonary embolism and serious cardiovascular disorders, including myocardial infarction. Only for post menopausal women with high risk for osteoporotic fractures. It reduces osteoclast activity & also increases osteoblast activity thus leading to new bone formation.
Teriparatide: Synthetic PTH
19
Q
Carbimazole
A
pro-drug as after absorption it is converted to the active form, methimazole. Methimazole prevents thyroid peroxidase enzyme from iodinating and coupling the tyrosine residues on thyroglobulin, hence reducing the production of the thyroid hormones T3 and T4 (thyroxine).
Treatment is usually given for 18–24 months followed by a trial withdraw. Block & replace pattern: carbimazole blocks thyroid hormone development and then needs to be given Levothyroxine while still on carbimazole.
SE: Bone marrow suppression, agranulocytosis (Watch for sore throat), flu like symptoms, Jaundice, Nausea, Headache, Pruritus, Taste disturbance
Cause cause aplasia cutis, hypothyroidism in fetus hence avoid in pregnancy.
Dose 15 mg titrate up.
20
Q
propyl Thiouracil
A
PTU inhibits the enzyme thyroperoxidase, which normally acts in thyroid hormone synthesis by oxidizing the anion iodide (I−) to iodine (I0), facilitating iodine’s addition to tyrosine residues on the hormone precursor thyroglobulin.
PTU also acts by inhibiting the enzyme 5’-deiodinase (tetraiodothyronine 5’ deiodinase), which converts T4 to the more active form T3. (This is in contrast to methimazole, which shares propylthiouracil’s central mechanism, but not its peripheral one.
Propylthiouracil is classified as Drug Class D in pregnancy. Class D signifies there is positive evidence of human fetal risk. The maternal benefit may outweigh fetal risk in life-threatening situations.[9] PTU is preferred over methimazole (which is also a class D) only in the first trimester of pregnancy and in women who may become pregnant because of the increased risk of teratogenicity of methimazole during critical organogenesis. In the second and third trimester, this risk is diminished and methimazole is preferred to avoid the risk of liver complications from PTU in the mother.
Its notable side effects include a risk of agranulocytosis and aplastic anemia, nephritis, SLE like symptoms, Hypo-prothrombinemia
Another life-threatening side effect is sudden, severe, fulminant liver failure resulting in death or the need for a liver transplantation, which occurs in up to 1 in 10,000 people taking propylthiouracil.
21
Q
Phosphodiesterase inhibitors,
11 subtypes
They relax and widens vessels
A
PDEi 03 = Milrinone (Heart, Vessels)
PDEi 04 = Roflumilast (Lungs)
PDEi 05 = Tadalafil (Lungs, Penis)
Pentoxyphylline- Theophylline is a non selective PDE inhibitor.
Milrinone: PDEi 3 - improves heart contraction, reduces platelet aggregation, has a role in limiting stroke
Rofflumilast: PDEi 5 = for COPD,
Crisaborole
Apremilast = for psoriasis, Ps arthritis
22
Q
Insulins
A
Rapid-Insulins:
Actions starts in minutes & Lasts for Hrs, Brand Name
1. Aspart: 5-15 min, 3-5 Hrs, NOVOLOG
2. Glulisine: 5-15min, 3-5 Hrs, APIDRA
3. Lispro: 5-15min, 4 Hrs, Humalog
4. inhaled: ultrarapid, AFREZZA
5. Regular: 30-60min, 6 Hrs, HUMULIN-R, NOVOLIN-R
Intermediate acting insulin:
Neutral Protamine Hagedorn insulin, also known as isophane insulin,
Insulin NPH: 3-4 Hrs, 16-24 Hrs, HUMULIN-No, NOVOLIN-N
Long acting insulins:
I. detemir: 24 Hrs action, LEVEMIR
I. Glargine: 24 Hrs action, LANTUS
23
Q
Anticholinergics:
substances that block the action of the neurotransmitter called acetylcholine (ACh) at synapses in the central and peripheral nervous system.
A
- Anti-muscarinics: = Atropine, Scopolamine, Hyoscine, Ipratropium, Tropicamide, Cyclopentolate, Pirenzepine, Dicyclomine, Doxylamine, Hydroxyzine, Glycopyrrolate, Mebeverine, Oxybutinin, Procyclidine, Solifenacin, Tiotropium, Tolterodine, Trihexyphenydil
-
Anti Nicotinics:
#Ganglionic Blocking: Hexamethonium, Mecamylamine, Trimethaphan
#Nondepolarizing neuromuscular blocking: Atracurium, Doxacurium, Mivacurium, Pancuronium, Tubocurarin, Vecuronium
#Depolarizing neuromuscular blocking: Succinylcholine
#Centrally acting nicotinic antagonists: 18-Methoxycoronaridine, Bupropion, Hydroxybupropion, Threohydrobupropion, Dextromethorphan, Dextrorphan, Methoxymorphinan
Hot as Hare - High fever
Dry as a bone - severe dehydration
Blind as a bat - blurred vision
Red as a beet - flushed skin
Mad as a hatter - Psychosis
24
Q
Complications of TPN
A
Short term:
Bleeding, Pneumothorax due to line, Line sepsis, Vein thrombosis, Hyperglycemia, refeeding syndrome, deranged LFT (Excess Nutrition)
Long Term: Sepsis, Line thrombosis, GB Stones, Renal stones, Bone disease
25
Adenosine
= blocks AV node conduction
= short acting, 10-15 seconds as rapidly metabolized by peripheral esterases
= Adenosine is used as an adjunct to thallium (TI 201) or technetium (Tc99m) myocardial perfusion scintigraphy (nuclear stress test) in patients unable to undergo adequate stress testing with exercise. "stress test", the dosage is typically 0.14 mg/kg/min, administered for 4 or 6 minutes, depending on the protocol.
SVT Dose - 6, 12, 12 mg
contra-indications: = Asthma, Sick sinus syndrome, AF+WPB together, Transplanted heart, Pt on-dipyridamole, Carbamazepine, Theophylline, and 2/3 degree CHB
Alternate SVT drug: Amiodarone, Flecainide, Verapamil, Metoprolol
26
Receptors with Agonist Actions
Alfa 1 = vasoconstriction
Beta 1 = inotrophic
Beta 2 = Vasodilation, Bronchodilation
Dopamine = vasodilation@ renal, splanchnic low doses, vasoconstriction at high doses
27
GM-CSF: Granulocyte Monocyte- Colony Stimulating Factor
- Sargramostim
- Molgramostim
is a monomeric glycoprotein secreted by macrophages, T cells, mast cells, natural killer cells, endothelial cells and fibroblasts that functions as a cytokine. The pharmaceutical analogs of naturally occurring GM-CSF are called sargramostim and molgramostim.
The human gene has been localized in close proximity to the interleukin 3 gene within a T helper type 2-associated cytokine gene cluster at chromosome region 5q31, which is known to be associated with interstitial deletions in the 5q- syndrome and acute myelogenous leukemia.
GM-CSF is found in high levels in joints with rheumatoid arthritis and blocking GM-CSF as a biological target may reduce the inflammation or damage. Some drugs (e.g. otilimab) are being developed to block GM-CSF.
28
Filgrastim: Granulocyte Colony Stimulating Factor (Neupogen)
= is a medication used to treat low neutrophil count.
= Common SE: fever, cough, chest pain, joint pain, vomiting, & hair loss.
= Severe SE: splenic rupture & allergic reactions.
Filgrastim is a recombinant form of the naturally occurring granulocyte colony-stimulating factor (G-CSF).
Neupogen is the name for recombinant methionyl human granulocyte colony stimulating factor (r-metHuG-CSF).
Other SE: include serious allergic reactions (including a rash over the whole body, shortness of breath, wheezing, dizziness, swelling around the mouth or eyes, fast pulse, and sweating), ruptured spleen (sometimes resulting in death), alveolar hemorrhage, acute respiratory distress syndrome, and hemoptysis.
Severe sickle cell crises, in some cases resulting in death, have been associated with the use of filgrastim in patients with sickle cell disorders.
29
High INR with warfarin-Management
> 8 INR with minor bleeding:
= Stop warfarin
= IV Phytomenadione, 1-3/5 mg slow
= Repeat if INR still high after 24 Hrs
= re start warfarin when INR < 5
> 8 INR with major bleeding:
= Stop warfarin
= IV Phytomenadione 5 mg slow iv
= Prothrombin complex dried, 25-50 mg/kg (contains 2, 7, 9, 10) - OR FFP 15 ml/kg
> 8 INR, no bleeding:
= Stop warfarin
= PO Phytomenadione 1-3 mg using same iv solution given orally
= re start Warfarin when INR < 5
30
Warfarin Information
Mechanism of Action
Warfarin competitively inhibits the vitamin K epoxide reductase complex 1 (VKORC1), an essential enzyme for activating the vitamin K available in the body. Through this mechanism, warfarin can deplete functional vitamin K reserves and thereby reduce the synthesis of active clotting factors. The hepatic synthesis of coagulation factors II, VII, IX, and X, as well as coagulation regulatory factors protein C and protein S, require the presence of vitamin K. Vitamin K is an essential cofactor for the synthesis of all of these vitamin K-dependent clotting factors.
FDA-approved clinical uses for warfarin:
Prophylaxis and treatment of venous thrombosis and arising pulmonary embolisms.
= Prophylaxis and treatment of thromboembolic complications from atrial fibrillation or cardiac valve replacement
= Reduction in the risk of death, recurrent myocardial infarction, and thromboembolic events (e.g., stroke, systemic embolization) after myocardial infarction
Off-Label clinical uses of warfarin include:
= Secondary prevention of recurrent stroke and transient ischemic attacks[4]
31
Warfarin Pharmacokinetics
Absorption: Rapid and complete absorption
The onset of action: The onset of action is typically 24 to 72 hours. A peak therapeutic effect is seen 5 to 7 days after initiation. However, the patient's international normalized ratio (INR) may increase within 36 to 72 hours after initiating treatment.
Duration of Action: 2 to 5 days
Distribution: Small volume of distribution (0.14 L/kg)
Protein Binding: 99%
Metabolism: Hepatic metabolism, primarily through the CYP2C9 enzyme. Other minor enzymatic pathways for metabolism include CYP2C8, 2C18, 2C19, 1A2, and 3A4.
Genomic Variants: Research has shown that genetic variations in CYP2C9 affect an individual's warfarin clearance. Patients who are heterozygous for the 2C9 (*1/*2 or *1/*3) can experience an approximately 37% reduction in S-warfarin clearance. Patients who are homozygous for reduced function alleles (*2/*2, *2/*3, or *3/*3) may experience a nearly 70% reduction in clearing S-warfarin.
Elimination Half-life: The half-life of warfarin is generally 20 to 60 hours (mean: 40 hours). However, it is highly variable among individuals.
32
Warfarin Sideffects
=Haemorrhage,
Rare cases of purple toe syndrome, warfarin-induced skin necrosis, and there are reports of calciphylaxis with warfarin therapy.
= Purple toe syndrome is a complication characterized by cholesterol microembolization that causes purple lesions to develop on the toes and sides of the feet. Purple toe syndrome usually develops 3 to 8 weeks after the initiation of warfarin therapy.
= Warfarin-induced skin necrosis is a serious condition in which subcutaneous tissue necrosis occurs due to an acquired protein C deficiency following treatment with warfarin. The risk of necrosis increases in patients with protein C or protein S deficiency. The skin necrosis usually occurs within the first week of therapy and management strategies, including discontinuing treatment with warfarin, administering fresh frozen plasma and vitamin K, and initiating anticoagulation therapy with either unfractionated heparin or low molecular weight heparin. = Calciphylaxis or calcium uremic arteriolopathy is another rare adverse effect in patients with or without end-stage renal disease.
33
Warfarin and Diet
While there is no specific diet recommended for patients on warfarin, certain foods and beverages can either limit or enhance the anticoagulant effect of warfarin. Vitamin K decreases the effectiveness of warfarin in the body. Therefore, the patient should receive education on maintaining a consistent dietary intake of vitamin K-containing foods.[15] Examples of high vitamin K foods include kale, green tea leaves, Brussel sprouts, and spinach. Other dietary recommendations include limiting the consumption of cranberry juice and alcohol while on warfarin therapy. Grapefruit juice and alcohol can enhance the anticoagulant effect of warfarin, thereby leading to increased bleeding complications
34
Dialysable Toxins
PLASMA-TV
- Phenobarbitol
- Lithium
- Acidosis
- Salicylates
- Metformin
- Alcohols
- Theophylline
- Valproic Acid
35
Substances amenable to multi-dose activated charcoal.
ABCDQ:
- Aminophylline / theophylline
- Barbiturates
- Carbamazepine / concretion forming drugs (salicylates)
- Dapsone
- Quinine
36
Substances that do not bind to charcoal.
PHAILS:
- Pesticides
- Heavy metals
- Acids/alkalis/alcohols
- Iron
- Lithium
- Solvents
37
Potentially lethal toxins where early activated charcoal may be indicated.
Killer C’s:
- Cyanide
- Colchicine
- Calcium channel blockers
- Cyclic antidepressants
- Cardiac glycosides
- Cyclopeptide mushrooms
- Cocaine
- Cicutoxin (water hemlock)
- Salicylates
38
Substances causing a wide anion-gap acidosis
CAT MUD PILES:
- Cyanide, carbon monoxide, colchicine
- Alcohol, alcoholic ketoacidosis, acetaminophen (in large doses)
- Toluene
- Methanol, metformin
- Uraemia
- Diabetic Ketoacidosis
- Paraldehyde
- Isoniazid, iron
- Lactic acidosis
- Ethylene glycol
- Salicylates
39
Substances that cause hypoventilation
SLOW:
- Sedative-hypnotics (barbiturates, benzodiazepines)
- Liquor (alcohols)
- Opioids
- Weed (marijuana)
40
Substances that cause hyperventilation.
PANT:
- PCP, paraquat pneumonitis, phosgene
- Acetylsalicylic acid (ASA) and other salicylates
- Noncardiogenic pulmonary oedema, nerve agents
- Toxin-induced metabolic acidosis
41
Substances causing hypertension.
CT SCAN:
- Cocaine
- Thyroid supplements
- Sympathomimetics
- Caffeine
- Anticholinergics, amphetamines
- Nicotine
42
Substances that cause hypotension
CRASH:
- Clonidine, calcium channel blockers
- Rodenticides (containing arsenic, cyanide)
- Antidepressants, aminophylline, antihypertensives
- Sedative-hypnotics
- Heroin or other opioids
43
Substances that cause hyperthermia.
NASA:
- Neuroleptic malignant syndrome, nicotine
- Antihistamines, alcohol withdrawal
- Salicylates, sympathomimetics, serotonin syndrome
- Anticholinergics, antidepressants, antipsychotics
44
Substances that cause hypothermia.
COOLS:
- Carbon monoxide
- Opioids
- Oral hypoglycaemics, insulin
- Liquor (alcohols)
- Sedative-hypnotics
45
Substances that cause tachycardia.
FAST:
- Free Base or other forms of cocaine, Freon
- Anticholinergics, antihistamines, antipsychotics, amphetamines, alcohol withdrawal
- Sympathomimetics (cocaine, caffeine, amphetamines, phencyclidine [PCP]), solvent abuse, strychnine
- Theophylline, tricyclic antidepressants, thyroid hormones
46
Substances that cause bradycardia
PACED:
- Propranolol (Beta blockers), poppies (opiates), propoxyphene, physostigmine
- Anticholinesterase drugs (I.e. cholinergics like physostigmine), antiarrythmics
- Clonidine, calcium channel blockers
- Ethanol or other alcohols
- Digoxin, digitalis
47
Anticholinergic
Blind as a bat;
Mad as a hatter;
Red as a beet;
Hot as Hades/Hell/Desert;
Dry as a bone;
The bowel and bladder lose their tone, and the heart runs alone.
Or…
Can’t See (blurred vision);
Can’t pee (urinary retention);
Can’t spit (dry mouth);
Can’t Shit (constipated)
48
Cholinergic Toxidrome
DUMBELLS:
- Diarrhoea, diaphoresis
- Urination
- Miosis
- Bradycardia
- Emesis
- Lacrimation
- Lethargic
- Salivation
49
Seizures
OTIS CAMPBELL:
- Organophosphates, oral hypoglycaemics
- Tricyclic antidepressants
- Isoniazid, insulin
- Sympathomimetics, strychnine, salicylates
- Camphor, cocaine, carbon monoxide, cyanide, chlorinated hydrocarbons
- Amphetamines, anticholinergics
- Methylxanthines (theophylline, caffeine), methanol
- Phencyclidine (PCP), propranolol
- Benzodiazepine withdrawal, botanicals (water hemlock, nicotine), bupropion, GHB
- Ethanol withdrawal, ethylene glycol
- Lithium, lidocaine
- Lead, lindane
50
Agents Causing Coma or Seizures
LETHARGIC:
- Lead, lithium
- Ethanol, ethylene glycol, ethchlorvyol
- Tricyclic antidepressants, thallium, toluene
- Heroin, hemlock, hepatic encephalopathy, heavy metals, hydrogen sulphide, hypoglycaemics
- Arsenic, antidepressants, anticonvulsants, antipsychotics, antihistamines
- Rohypnol (sedative hypnotics), risperidone
- Gamma-hydroxybutyrate (GHB)
- Isoniazid, insulin
- Carbon monoxide, cyanide, clonidine
51
Agents Affecting Pupil Size
Miosis (COPS)
Cholinergic, clonidine, carbamates
Opioids, organophosphates
Phenothiazines (antipsychotics), pilocarpine, pontine haemorrhage
Sedative – hypnotics
Mydriasis (SAW)
Sympathomimetics
Anticholinergics
Withdrawal syndromes
52
Lithium Toxicity
Dose Limit < 1800 mg/Day
Signs: Tremors - fine to course, Clonus, Confusion, Coma, Death
PPT: dehydration and Co-drugs: STAND: SSRI-Theophylline - ACEi-NSAIDs-Diuretics)
It can cause nephrogenic DI with kidneys resistant to ADH action (Hyponatremia due to excess water in body retained)
Lithium to monitor 12 Hrs after first dose and twice weekly then monthly
Acute Goal: 0.8 - 1.2 mEq/Lit
Maintain: 0.8 -1 mEq/Lit
Rx: Hydration, Dialysis
53
Drugs that cause Gastric Ulcers
NSAIDs,
Corticosteroids
Biphosphonates
Illicit drug use
Aspirin
Potassium chloride
Mycophenolate
Non Drugs Causes:
Helicobacter pylori infection
Crohn's disease or UC
Zollinger Ellison syn (Gastrinoma)
Radiation therapy to area
Chemotherapies
Neuhauser Syndrome: rare autosomal recessive congenital disorder that presents with megalocornea, mental retardation, hypotonia, and facial dysmorphism, peptic ulcers, tremors, mastocytosis (excess mast cells)
54
Drugs Causing pancreatitis
Azathioprine
Statins
Didanosine
Asparginase
Valproate
Antimonials
Pentamidine
Mercaptopurines
Thiazides, Frusemide
Co-trimoxazole
Less common:
Rifampicin, Octerotide, Carbamazepine, Acetaminophen, IFN, Enalapril, Cisplatin, Erythromycin
55
Drugs causing lupus
Procainamide
Hydralazine
Isoniazid
Diltiazem
Penicillamine
56
Radioactive Iodine, I-131
Made by John Livingston and Seaberg, 1938, California
Half Life: 8 days
High dose can induce cancers
Medical Dose: 400-600 mbg (megabequerals) capsule/liquid
Can cause initial thyroiditis symptoms
Advice:
- no sexual contacts for 1 month
- no pregnancy attempts for 6 months after
- one week isolation recommended
its byproduct of uranium/Plutonium fission
I-MIBG scan uses it for Pheochromocytoma/ Neuroblastoma diagnosis
Reacts with chlorine bleech and can release elemental iodine gas
Iodine is a chemical element with the symbol I and atomic number 53. The heaviest of the stable halogens, it exists as a semi-lustrous, non-metallic solid at standard conditions that melts to form a deep violet liquid at 114 °C (237 °F), and boils to a violet gas at 184 °C (363 °F).
57
Carbimazole
Prodrug of methimazole, 10 mg gives 6 mg
Inhibits thyroid peroxidase (TPO) which inhibits organification of iodine molecule into hormone
Side effects:
Agranulocytosis, Fever, Rash, Cholestasis (jaundice)
also reduces thyroid stimulating antibodies after use
takes about a month for TFT improvement
Add:
Propranolol at start of therapy 80 mg TID - taper after 4 weeks tp 40 mg TID = taper after 4 wks to 40 mg BD and then STOP
58
Nirmatrelvir/Ritonavir for Covid19
Nirmatrelvir/ritonavir (Paxlovid) is a combination of two protease inhibitors, nirmatrelvir and ritonavir.
Nirmatrelvir is a 3C-like protease inhibitor that interacts with the main viral protease of SARS-CoV-2, which cleaves the SARS-CoV-2 polyprotein into non-structural proteins. This represents a fundamental step in the viral replication and assembly of new viral particles.
Ritonavir is a protease inhibitor with very minimal antiviral activity. Ritonavir is a strong inhibitor of the cytochrome P450 (CYP) 3A4, and acts as a boosting agent, by increasing the concentration of nirmatrelvir.
Nirmatrelvir/ritonavir has many drug to drug interactions, mainly caused by ritonavir.
Some medications that are contraindicated with nirmatrelvir/ritonavir include: antiepileptics, anticoagulants, antibiotics (rifampicin), antiarrhythmics, antipsychotics, and immunosuppressants.
Nirmatrelvir/ritonavir is also contraindicated in patients with eGFR <30 mL/min.
59
Molnupivir
Molnupinavir is a synthetic ribonucleotide analogue (N4-hydroxicytidine) which binds to the viral RNA-dependent RNA-polymerase and inhibits viral replications by introducing copying errors.
60
Remdesivir
Remdesivir is a prodrug of an adenosine C-nucleoside, which inhibits viral replication by interacting with the RNA-dependent RNA-polymerase.
Remdesivir is contraindicated in patients with eGFR <30 mL/min. It is also contraindicated in patients with severe hepatic dysfunction or ALT >5 times the upper limit of normal.
61
Tocilizumab, Sarilumab, Baricitinib
Tcilizumab, sarilumab, baricitinib and other anti-inflammatory medications are used in some countries in people with severe COVID-19 in addition to dexamethasone to manage the hyperinflammatory syndrome.
Anti-inflammatory medications do not act directly against the virus, but they modulate the immune response to the virus, which is responsible for the organ damage due to the hyperinflammatory response in severe COVID-19.
62
Good CSF penetrating Drugs
Fluoroquinolones
Trimepthoprin-sulfamethoxazole
Metronidazole
Chloramphenicol
Fosfomycin
Isoniazid
Pyrazinamide
Voriconazole/fluconazole
Pyrimethamine
Albendazole/praziquantel
63
Good penetration only in inflamed meninges
Glycopeptides (vancomycin)
Macrolides (azithromycin)
Rifamp(ic)in
Ethambutol
64
Poor penetration of the CSF
Beta-lactams¹
Aminoglycosides
Tetracyclines (doxy, tigecycline)
Clindamycin
Daptomycin
Colistin
Amphotericin B
Echinocandins
Itraconazole/posaconazole
65
Drugs causing Optic neuropathy
Isoniazid, Ethambutol
Vincristine, Cisplatin
Ciclosporine
Disulfiram
Sildenaphil
Amiodarone
Diplopia causing drugs: Phenytoin, Topiramate, Carbamazepine
Other causes: B12, folate deficiency, DM, MS, Graves ophthalmopathy, Amaurosis fugax, Lead, CO exposure, Methanol blindness
66
Sumatriptan
used in acute attack of migraine as subcut injection, 6 mg or oral 25-100 mg. antagonist to serotonin receptors. It can cause acute chest syndrome, STEMI, Strokes as vasoconstrictor.
Do not use with complex migraine ie with neurological deficits. Also avoid Beta blockers and OCPs
67
Mechanisms of Anticonvulsants
Inhibition of Na dependant Action potentials: Phenytoin, Mazetol, Lamotrigine, Topiramate, Zonisamide
Inhibition of voltage gated Ca channels: Phenytoin
Decrease in Glutamate release: Lamotrigine
Increase GABA availability: Valium, Barbiturates
Modulation of Synaptic Vesicle release: through binding to the synaptic vesicle protein SV2A in the brain: = Levetiracetam (keppra)
68
Drugs causing convulsions
Alkylating: Busulfan, Chlorambucil
Antimalarials: Chloroquin, Mefloquin
AntiMicrobials: Ceftriaxone,
Quinolones, Acyclovir, INH
Anaesthetics: Meperedine, Tramadol, Local anaesthesia
Dietary supplements: Ephedra, Gingko
Immunomodulators: Ciclosporine, OKT3, Tacrolimus, IFN
Psychotropics: Antidepressants, Lithium, AntiPsychotics
Sedatives-Hypnotic withdrawals: Alcohol, Barbiturates, Valium
Drugs of Abuse: Cocaine, Amphetamines, Phencyclidine,
Others: Theophylline, Contrast agents, Flummazenil
69
Drugs causing headache
Nitrates
Calcium channel blockers
Tetracycline
Vitamin A derivatives
Analgesic overuse
Cocaine, Steroids,
Nicotine withdrawal
70
Acquired pendular nysagmus
may affect one or both eyes, and can occur in any axis or combination of axes. Although acquired pendular nystagmus may be idiopathic, the most common cause of secondary acquired pendular nystagmus is disorders of central myelin, namely multiple sclerosis (MS).J
71
Drugs causing Tremors:
Resting tremor causing drugs:
= Metoclopramide, Prochlorperazine
= Chlorpromazine, Haloperidol
Intention tremor causing drugs:
= Lithium toxicity
= Phenytoin, Valproate
Physiological tremor causing drugs:
= Salbutamol
= Theophylline
= Tricyclic antidepressants,
= Corticosteroids
= Thyroxine
Recreational drugs causing tremors:
= Cocaine, Amphetamines, Anabolics
Toxins causing Tremors:
= Heavy metals
= Organophosphates
72
Anti TNF drugs
for conditions:
Juvenile idiopathic arthritis, RA, Psoriatic arthropathy, Psoriasis, Ankylosing spondylitis, Crohn's disease
Agents:
Infliximab, Etanercept, Adalimumab
Side Effects:
TB reactivation, Leukemias, Lymphomas, Nausea, Worsening CCF, Hypersensitivity reactions, Anemia, Aplastic anemia, low platelets
Contra-indications:
Pregnancy, Breast feeding, Active bacterial infections, Active TB, Latent TB, Septic arthritis, CCF, Demyelinating disease
73
Amiodarone Side Effects
Nausea, Metallic taste in mouth, Nightmares, Tremors, Headaches, Rashes, Phototoxicity
Optic neuritis
Peripheral neuropathy
Myopathy weakness
Hepatitis, cirrhosis
Interstitial lumb fibrosis
Hyper or Hypothyroidism
Corneal microdeposits: Night Glares
Epididymitis
Cardiac arrhythmias
74
Anti Arrhythmic Classification
Class 1 -
Interferes with sodium channel,
1a - Quinidine, Procainamide
1b - Lidocaine, Phenytoin, Mexilitine
1c - Flecainide, Encainide, Moricizine
Class 2 -
Anti sympathetic nerves: Beta blockers
Class 3 -
affects K efflux: Amiodarone, Sotalol, Ibutilide, Dofetilide, Dronedarone
Class 4 -
Affects Ca++ channel and AV nodes
Verapamil, Diltiazem
Class 5 - unknown or some other mechanism
Adenosine, Digoxin, Magnesium sulfate
75
Bismuth Subsalicylate
Bismuth subsalicylate is used to treat diarrhea in adults and teenagers. It is also used to relieve the symptoms of an upset stomach, such as heartburn, indigestion, and nausea in adults and teenagers.
You should not use bismuth subsalicylate if you have bleeding problems, a stomach ulcer, blood in your stools, or if you are allergic to aspirin or other salicylates. Using this medicine in a child or teenager with flu symptoms or chickenpox can cause a serious or fatal condition called Reye's syndrome.
Bismuth subsalicylate is contraindicated in pregnancy because of associations with premature fetal ductus arteriosus and intrauterine growth problems.
76
Local Lidocaine dosing
Actions starts in 5-10 minutes
Action lasts 1-2 hours without adrenaline mix and 2-4 Hours with adrenaline
Dose:
3 mg/kg plain
7 mg/kg with adrenaline
77
Methyl Pred in spine trauma
78
Bupropion
Anti smoking medicación
Does - 150-300 mg per day
Acts - by boosting Brain levels of dopamine and norepinephrine
Mimics nicotine
Contraindicated with seizures
79
Evolocumab
Alirocumab
Antilipidemic monoclonal antibodies
Lowers LDL cholesterol
Binds proprotein convertase subtilisin kexin type 9 (PCSK9 inhibitors) which decreases degradation of LDL receptors thus helping their pick up and clearance
80
Medicacions to treat Weight Loss
1. Apettite stimulants:
Corticosteroids, Progestational agents, Dronabimol, Serotonin antagonists (cyproheptadine)
2. Anabolic agents:
Growth hormone & testosterone derivatives
3. Anti catabolic agents:
Omega 3-Fatty acids, Pentoxyphylline, Hydrazine sulfate, Thalidomide
81
Phenazopyridine
An azo dye, a urinary analgesic, acts on urinary mucosa for local analgesia.
- 100-200 mg TDS after meals
- can cause orange ursine, tears, lenses
- can cause haemolytic anemia in G6PD deficiency
- can cause AKI, methemoglninemia
82
Acetylcholine esterase inhibitors
Used in moderate **Dementia**
**Donepezil**- 5 mg start, 10 mg max
**Galantamine**- 4 mg bd, 12 mg bd max
**Rivastigmine** - 1.5 mg bd, 6 mg bd max
**Side effects**
Diarrhea, nausea, anorexia
Weight loss
Syncope
83
Memantine
A NMDA antagonist
Used for dementia
Dose - 5 mg BD to 10 mg BD
84
Antivirals for Flu
Oseltamivir > 14 days old
Zanamivir (Relenza) - inhaled powder, > 7 days older, not in asthma/COPD
Peramivir (Rapivab) - IV only, > 6 months
Baloxavir (Xofluza) - single dose pill, not if pregnant or breastfeeding
85
Medications for **urge incontinence**
(detrusor overactivity)
**Tolterodine** - short/long acting
**Oxybutynin** - short/long acting/skinpatch
**Fesoterodine**
**Trospium chloride**
**Darifenacin**
**Solifenacin**
**Mirabegron** - beta 3 agonist, 25/50 mg PO OD
** Onabotulinum toxin A** injection into detrusor muscle
86
Anti emetic medications
Metoclopramide
Scopolamine- transdermal, 1.5mg/3days
Dexamethasone, 20 mg Divided
Diphenhydramine, 25 mg TDS
Lorazepam 0.5-1 mg
Ondansetron
Granisetron
Dolasetron
Palonosetron
Aprepitant (neurokinin-1 receptor antagonists)
Fosaprepitant
Rolapitant
Netupitant (N-receptor antagonist)
Olanzapine
Prochlorperazine
Mirtazapine
Dronabinol
87
Na Channel Blockers causing ECG effects
these are contra-indicated in Brugada syndrome
Tricyclic antidepressants (TCA's)
Type Ia anti arrhythmics: Quinidine, Procainamide
Type Ic anti arrhythmics: Flecainie, Encainide
Local Anaesthetics: Bupivacaine, Ropicavaine
Antimalarials: Chloroquin, OH-chloroquin
Dextropropoxyphene (Opiod analgesics)
Propranolol
Carbamazepine
Quinine
88
Long acting Opioids
- Morphine - Oral Sustained release
- Hydromorphone, OD
- Oxymorphone, BID
- Oxycodone, BID, TID
- Hydrocodone, BD
- Methadone 3/4 times a day
89
Buprenorphine
Long acting, available as Oral, Patch, Parenteral, buccal formulations, Less addictive risk, Less risk of respiratory depression or sedation,
Skin Patch -5/10/20 mgc/Hr release
IV dose - 300 mcg, repeat after 60 min
IM dose -600 mcg once
Buccal dose - 150-450 mcg BD, max 900 mcg/Day
**Subutex**: sublingual tablet
**Suboxone**: sublingual film
**Probuphine**: subdermal implant
**Sublocade**: Subcute depot injection
90
Opioid induced Neuro-toxicity
occurs in patients on high dose opioids and can have manifestations as:
**Hallucinations** or **Delirium** - manage with Haloperidol
**Hyperalgesia** : increased pain to light touch (**Allodynia**), might resolve with **Opioid Rotation** or lowering dose but takes time.
**Myoclonus**: - can manage with small doses of clonazepam, baclofen, Gabapentin.
91
Medications to treat neuropathic pain
92
Neuropathic analgesic tips
1. Gabapentin, Pregabalin: are Ca channel Alfa-2-delta ligands: can cause sedation, dizziness, ataxia: need renal adjustments
2. Duloxetin, Venlafaxin - are Serotonin Norepinephrine reuptake inhibitors SNRIs. Duloxetine to take full stomach to avoid nausea, Venlafaxine can cause HTN & ECG changes.
3. Nortryptiline & Desipramine are preferred over amitryptiline - as causes less orthostatic hypotension & less anticholinergic side effects.
4. TCAs and SNRIs should not be prescribed together due to risk of serotonin syndrome
5. Topical 5% Lignocaine and Capsaicin 8% patches are second line.
93
Managing Opioid induced **nausea**
Options:
1. Haloperidol: 0.5-4 mg PO/Sq/IV
2. Prochlorperazine: 10mg PO/IV or 25 rectal 6 hrly
3. Ondansetron: 4-8 mg PO or IV QDS
4. Mirtazapine
5. Medical cannabis
94
NOAC contra-indications
- CKD, GFR < 15 for factor Xa inhibitors
- GFR < 30 for Dabigatran, anti IIa
- Pregnancy, Lactation
- Metal cardiac valves
95
Heparin
Anti factor IIa and axa
Routes - IV or subcute
Monitor - aPTT, anti-Xa, anti-IIa
SideEffects - Platelet drop, bleeding
Antidote - Protamine sulfate: 1 mg neutralises 100 Unit heparin
96
Cryoprecipitate
Cryoprecipitate is the part of plasma that contains a number of clotting proteins (factors) that help control bleeding. It's made by thawing fresh frozen plasma (FFP) between 1 and 6˚C and then collecting the cold-insoluble proteins (precipitate).
**Contents**: fibrinogen, fibronectin, clotting factors 8, 13, von willebrand factor
97
TNF inhibitors
Used in psoriasis treatment:
1. Infliximab- most rapid response and used in severe form like pustular or erythrodermic type
2. Etanercept: used for long term treatment as 50 mg subcute twice weekly 3 months then once weekly
3. Adalimumab (Humira):
98
Apremilast
Oral PDE 4 inhibitor,
Can be used long term for
Plaque type psoriasis, Needs no monitoring
Other options:
*TNF inhibitors
*IL-12/23 monoclonal antibodies: like Ustekinumab, Guselkumab
*Janus kinase JK inhibitors: Tofacitinib
*IL-17 monoclonal antibodies: Secukinumab, Brodalumab, Ixekizumab,
99
Skin protectives: **Calamine**
**Calamine** Calamine USP XVIII is zinc oxide (ZnO) with a small proportion of ferric oxide (FezO, iron(IlI)oxide). • It contains not less than 98% and not more than 100.5% of ZnO.
• Preparation: - The official calamine is obtained by calcination (powdered by heating) of the natural ore. - The calcined product is then passed through a 100-mesh sieve to get a
finely powdered material for good adhesive and cohesive properties.
• Properties:
- fine, pink powder
- odorless and tasteless
- insoluble in water but soluble in mineral acids Uses: - topical protective used in dusting powders, ointments & lotions
for its soothing, adsorbent properties.
100
Skin protectives: Talc
Talc USP XVIII is hydrated magnesium silicate. Contains 28.1% to 31.2 % MgO, 57 to 61.7% SiOz, 3 to 7% H20
Properties:
- Very fine white or grayish white crystalline powder.
- Smooth, greasy feeling to the touch (unctuous)
- Adheres readily to the skin
- Free from grittiness
- odorless, tasteless, insoluble and chemically inert
- low adsorptive properties
• Uses: - useful as a lubricating, protective dusting powder
- as a filtering aid
101
Calamine Forms:
Popular form of calamine:
**Calamine lotion USP XVIII** that contains equal quantities of Calamine and Zinc Oxide suspended with the aid of Bentonite Magma in calcium hydroxide solution. It is a protective, with good drying effect and mild
astringent action.
**Phenolated Calamine lotion** USP XVIII contains 1% liquified phenol that provides local anesthetic and antipruritic action (anti itching action).
102
Skin protectives: Titanium dioxide
**Titanium Dioxide**
Titanium Dioxide USP XVIII is a white, amorphous, odorless, tasteless, infusible powder.
• Neutral to litmus • Insoluble in water, HCl, nitric acid but soluble in hydrofluoric acid
Uses :
• Topical protective
Used in sun creams and sun screen products for its opacity. Its high refractive index (2.7) is useful for screening out ultraviolet radiation.
• White pigment in cosmetics
103
Colostomy protective: Aluminium
**Aluminium**
Properties :
• Aluminium USP XVIII is a fine, free-flowing silvery powder
• Free from gritty or powdered particles • May react with atmospheric oxygen to form a layer of aluminium
oxide Al that protect it from further oxidation
• Insoluble in water, alcohol, nitric acid and sulfuric acid
Uses : present in 10% concentration in aluminium paste using zine oxide as the ointment base as a protective to prevent irritation around intestinal fistulae As a protective around the colostomy opening after surgery for
intestinal cancer.
104
Skin protectives:
Simethicone/dimethicone
**Simethicone / Dimethicone**
• It is a silicone polymer, known generally as silicone oils
• Inert, protective substance
• Occurs in liquid form • Adhere very well to the skin but exclude contact with air so must not be applied on broken skin/ wounds that requires drainage.
• Used in ointments and creams for application to the skin as a water repellant and protective against contact irritants. usual concentration in these preparations: 30%
105
Oxidative antimicrobials: H2O2
Hydrogen Peroxide Solution USP XVIII
Clear, colourless liquid
Contains not less than 2.5g and not more than 3.5g of H,0z
Decomposes in contact with many oxidizing and reducing agents and
metal contaminants
Acid to litmus
Miscible in all proportions with water, alcohol or ether
Complexing or chelating agents (e.g. acetanilide 0.02 - 0.05%) are used
to stabilize them.
It is a weak acid in aqueous solution, ionizing primarily to form the
peroxide ion
H02 > 2H++ 02°
106
H2O2 uses
H2O2: Used as a mild oxidizing antiseptic in contact with open or
abraded tissue, exposing the chemical to the enzyme, catalase. Catalase causes decomposition of H,, to water and oxygen.
2H20г →> 2H20 + 02 •
The foaming release of oxygen provides mechanical cleansing action to remove dirt, bacteria, debris from the surface of the wound.
When diluted with one part of water it can be used as a gargle or mouthwash for the treatment of throat and mouth infections.
107
Oxidative antimicrobials: Zinc oxide
**Zine Peroxide USP XVII:**
White or faintly yellow fine odorless powder Insoluble in water and organic solvents
Unstable at temperatures above 140° C It will dissolve in dilute acids with decomposition to a soluble zinc salt and hydrogen peroxide.
Zn02 + 2HCl -> ZnCh + H20г
108
Zinc oxide uses
Used as an antibacterial and mild astringent • Although it appears to be insoluble in water, it will slowly hydrolyze to zine oxide and hydrogen peroxide. slow
**ZnO + H20 - ZnO + H20z**
room temperature
This reaction is responsible for its antibacterial action in that the hydrogen peroxide under the influence of catalase will release oxygen at the site of infection. The remaining zine oxide will exert an astringent action.
A 25% suspension or direct application of the powder may be used
to treat mouth infections caused by anaerobic microorganisms.
109
Oxidative antimicrobials: Na perborate
**Sodium Perborate**
• 86.5% NaBO3.4H,0
• No longer official but was official in N.F XII
• White cystalline granules/powder
• Hydrolyses slowly to sodium metaborate (NaBO,) & hydrogen peroxide
NaBO3 4H20 -→> NaBO, + H20 + 3H20
• Basic in nature of solution is due to formation of NaOH
NaBO,+ H20 - > NaOH + H,В03
Uses:
• As an antiseptic in the treatment of oral infections (as a paste with glycerin or water or freshly prepared 2% mouthwash). Used in powdered or dry dentrifice in concentrations of 10 to 20% (disadvantage: hydrolysis of particles will produce NaOH that will corrode enamel or gum tissue).
110
Oxidative antimicrobials: KMnO4
Potassium Permanganate USP XVIII (KMnO,)
• Odorless, dark purple crystalline compound
• Soluble in water • When heated at 240° C, it decomposes with the liberation of oxygen, leaving manganese oxide (MnO,)
and potassium manganate (KMnO,).
• Strong oxidizing agent both in dry state and in solution • Great care must be taken in handling it as dangerous explosives may occur if it is brought in contact with organic or readily oxidizable substances, either in
solution or in dry state.
(KMnO,) • Acid solutions of potassium permanganate reduces the permanganate ion (MnO, / Mn+7) to the manganous ion
with the evolution of oxygen.
2KMn04 + 3H,SO4 →> K,SO4+2MnSO4+3H20+5[0] • Neutral or alkaline solution produces a brown precipitate
of manganese dioxide (MnO,).
2KMn04 + H20 →> 2Mn02 + 2KOH + 3[0] • The antibacterial action is dependant upon its oxidation of protein or other bioorganic substances. The oxygen
released is the effective agent.
111
KMnO4 uses
Used for both their antibacterial and antifungal actions • Used externally in concentrations ranging from 0.2% to
about 0.006%. • Used for skin infections (dermatitis) caused by bacteria and fungi and for poisoning produced by plant and
animal toxins. • Used in the treatment of vesicular (small blisters/raised areas containing fluids) stage of eczema, tinea pedis
(fungal infection of the foot).
112
Oxidative antimicrobials: Na Hypochlorite
Sodium Hypochlorite Solution N.F. XIII (Dakin's
solution)
• NaOCl is very unstable and usually found only in solutions
• Contains not less than 4% and not more than 6% by weight of
NaOCl
• Clear, pale greenish yellow liquid having an odor of chlorine
• Has an alkaline pH coloring red litmus blue • Not suitable for application to wounds since its alkalinity and
oxidizing action is too strong for use on tissues
• In addition, the solution dissolves blood clots and delays healing • A diluted form is known as Labaraque's solution and consists of Sodium Hypochlorite Solution that has been diluted with an equal
volume of water (approx. 2.5% NaOCI)
This solution is used a disinfectant on inanimate (nonliving)
113
Sodium Hypochlorite uses
Useful as a disinfectant and laundry bleach • Effective as an germicidal agent that can be used to disinfect areas, instruments and utensils exposed to pathogenic
microorganisms
• Diluted form is used as a mouthwash
Disadvantages: • Dissolves sutures and blood clots and prolongs clotting time, can lead to secondary hemorrhage • Instability of solution requires storage in tight, light-resistant containers and avoidance of excessive heat.
114
Oxidative antimicrobials: iodine
Properties of iodine: • Occurs in the form of heavy, grayish black plates or granules, having a
metallic luster
• Has a characteristic penetrating odor • Very slightly soluble in water (1 in 2950), soluble in alcohol (1 in 12.5) and in solutions of iodides (I-) and freely soluble in carbon disulfide
and chloroform. Both iodide and triiodide ions (I3- )are devoid of antibacterial activity although triiodide ions can revert to I, and I thus retaining
antibacterial potency. It is a mild oxidizing agent. The oxidizing action is mediated through formation of hypoiodous acid (HIO)
I2 +Hz0 -> HI+ HIO -->HI+ (0)
-——-
Free iodine is about six times more effective than hypoiodous acid,
HIO.
It will oxidize iron to form ferrous iodide.
Fe + 12 - > FeIz For this reason metal spatulas should not be used to handle iodine and balance pans should be protected against pitting by using weighing
papers. Preparations providing free iodine are bactericidal, fungicidal,
amebicidal and virucidal. • lodine is very effective in dilute solution e.g. a 1:20000 concentration
will kill most bacteria in one minute and bacterial spores in 15 minutes. • Iodine is easily inactivated by organic materials in GIT so very little
iodine is absorbed. • Ingestion of large quantities of iodine will have a corrosive action producing abdominal pain, gastroenteritis and possible bloody
diarrhea. Treatment: gastric lavage with a soluble starch solution or
administration of a 5% sodium thiosulfate solution.
115
Iodine solutions
Iodine Preparations and Compounds :
• Iodine Solution N.F XIII
• Iodine Tincture U.S.P. XVIII
• Both the solutions contain the same concentration of ingredients. • In each 100ml they contain not less than 1.8g and not more than 2.2g of iodine (I) and not less than 2.1g and not more than 2.6g of sodium iodide (Nal). They differ only in the nature of the solvent i.e. - Iodine solution is aqueous, having being prepared with purified water, and Iodine
Tincture contains approximately 50% alcohol as the final solvent.
• Both solutions are transparent, reddish brown in color
• Iodine solution has the characteristic odor of iodine • Iodine Tincture has the characteristic odor of iodine as well as theodor of alcohol • The active antimicrobial agent common to both of thesepreparations is iodine.
Uses of Iodine Tincture and lodine Solution :
• Effective topical antiseptic agents • Used as antiseptics on the skin prior to surgery - Iodine Tincture is more suitable for this purpose as the alcohol can improve the penetration of the iodine due to a wetting or spreading effect and also provides additional
antibacterial effect. • Can be diluted with water for applications to wounds and abrasions - Iodine solution is preferred since the alcohol in the tincture is very irritating to the open tissues and
causes stinging when applied to wounds.
116
Povidone iodine
Povidone-Iodine is a complex of iodine with Povidone N.F XIII which is a polymer also known as polyvinylpyrrolidone or
PVP. • Both the aerosol and solution contains not less than 85% and
not more than 120% of the labeled amount of iodine.
Povidone-lodine is a member of a class of compounds
referred to as iodophors. • Iodophors are complexes of iodine with carrier organic molecules serving as a solubilizing agent. These complexes
slowly liberate iodine in solution. Advantages of Povidone-Iodine complex over elemental
iodine solutions:
Nonirritating effect on tissues
• Its comparatively low oral toxicity
• Water solubility • Low iodine vapor pressure making it stable to possible iodine
loss
• Nonstaining and can be washed clear from skin & clothing.
• The complex is a yellowish brown amorphous powder
• Has a slight characteristic odor
• Acid to litmus • Soluble in water and in alcohol and insoluble in organic
solvents. The Povidone- Iodine solution is a transparent liquid having a
reddish brown color and a pH of not more than 6.
117
Povidone iodine uses
Lack of tissue irritation makes it useful for application to sensitive areas and mucous
membranes • Recommended for surgical scrubs and preoperative
antisepsis of the skin
• Used in gargles and mouthwashes Examples: Betadine solution (concentrations of
0.1% to 1% of available iodine).
118
Protein precipitant: Antimicrobials: Silver nitrate
Colorless or white crystals which become gray or grayish black on exposure to light in the presence of
organic matter • Very soluble in water, sparingly soluble in alcohol and freely soluble in boiling alcohol • pH of 1% solutions is between 4.5 and 6 and must be clear or colourless • Solutions of silver nitrate in concentrations between 0.5 and 1% are used as antibacterial agents.
When a protein solution is treated with a solution containing a soluble silver salt, a heavy precipitate is formed involving a complex interaction
between the silver ions and protein. • This type of reaction is the basis for the antimicrobial action of the silver
compounds. The protein precipitant action of silver ion is not selective i.e. it will
precipitate both bacterial and human proteins.
Siter ion eipt to protein pes inerations between the
COOH, -NH, and heterocyclic residues eg histidine. When applied to tissue in a concentration of 0.1% silver the activity is
rapidly bactericidal Sustained action: A bactericidal action continues after the initial application due to the slow production of silver ions from the silver
proteinate and silver chloride. This sustained action at the tissue levels has given rise to colloidal
products of silver proteinate and halide as antibacterials.
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Silver nitrate
Silver has oligodynamic action, meaning it is active in small quantities. Silver preparations are bacteriostatic at concentrations of silver ion below that required for protein precipitation. Solutions of silver nitrate are bacteriostatic at concentration of 1:30,000 and bactericidal at 1:4000 in the presence of organic matter. • Irritation of the skin becomes a factor at concentrations above 1:1000. Extended use of silver preparations causes a darkening of the skin due to the deposition of free silver below the-Epidermis a condition known as **argyria.**
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Silver nitrate uses
Employed as an antibacterial in solutions ranging from 0.01 to 10% (higher concentration present astringent and irritant properties to the tissues). • Used in concentration of about 1:10,000 on sensitive membranes e.g. **irrigation of
the urethra and bladder.**
• Used in treatment of **infected ulcers in the mouth** (10% solution of silver nitrate). • Silver Nitrate **Opthalmic solution** U.S.P XVIll is a 1% solution for instillation into the eyes of newborn babies.
• Used as a prophylactic measure against infections caused by gonococcal organisms. • 0.5% aqueous solution of silver nitrate is used in the form of wet dressing on burnec
areas of patients suffering from third-degree burns. This form of therapy involves the mechanism of sustained action in that the silver ions are precipitated by tissue protein and chloride ion. The antibacterial activity is then dependant upon a low but minimal concentration of ions in equilibrium with
the insoluble forms. This is a good initial treatment due to both the antibacterial effect and the reduction
in fluid evaporation and the heat loss produced by the wet dressing. Side effects of this treatment: electrolyte imbalance due to precipitation of chloride such as low serum sodium, metabolic acidosis and diarrhea.
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Mild Silver protein solution
Mild Silver Protein N.F XIII : • The solution employed as antibacterial agents may range in
concentration from 0.5 to 20%. • Increase in dilution increases the release of ionized silver and this
increases irritation. • Calcium sodium EDTA at a concentration of 10mg/ml (1%) may be used to stabilize the solutions. It acts by chelating the silver ions released, thereby preventing the physical breakdown of the colloidal
solution and maintaining the low irritant action of the product.
Uses of Mild Silver Protein N.F XIII :
• Provide bacteriostatic action • Due to their low irritability they are used as local antibacterials on
mucous membranes in the nose, throat and conjuctiva of the eye
• Used to irrigate the urethra and bladder
• Treatment of gonococcal infections e g gonococcal conjuctivitis
Other colloidal silver preparations: Colloidal AgI, AgCl
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Yellow mercury compounds
**Yellow Mercuric Oxide N.F XIII (HgO)**
• Yellow to orange-yellow, heavy, impalpable powder
• Odorless and stable in air
• Practically insoluble in water and alcohol • Readily soluble in diluted hydrochloric acid and nitric acid forming colorless solutions On exposure to light, red form of mercuric oxide forms (no longer official) • When heated it will decompose to metallic mercury and oxygen.
Uses of Yellow Mercuric Oxide: It slowly releases Hg+ providing a mild sustained antbacterial
effect.
• So it is used in Yellow Mercuric Oxide Ophthalmic Ointment
N.F. XIII that contains between 0.9 and 1.1% of HgO. It is used treat mild infections and inflammation of the eye
including conjuctivitis.
• can also used for treating fungal infections of the skin. Caution: the ointment must not come in contact with metallic containers except those made of stainless steel, tin or tin- coated material to avoid formation of free mercury and development of small metallic particles that may be
damaging to the eye.
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Ammoniated mercury
**Ammoniated Mercury U.S.P XVIII** Hg(NH,)Cl • White, pulverulent (easily powdered) pieces or white,
amorphous powder
• Odorless, stable in air but darkens on exposure to light • Insoluble in water and alcohol but readily dissolves in
warm hydrochloric, nitric and acetic acids. Although insoluble, prolonged contact with water will cause the formation of a yellow basic compound having the formula H,N(HgO)HgCl. This necessitates the use of oil in lotions containing this compound. Ammoniated Mercury Ointment U.S.P XVIII contains between 4.5% and 5.5% of Ammoniated Mercury.
**Uses of Ammoniated Mercury**
• It is mildly antiseptic and is used primarily in ointments. • Used in the treatment of impetigo contagiosa and
fungal infections of the skin (dermatomycoses).
• Used in the treatment of crab louse infestations.
• Available as 5% and 3% ophthalmic ointment.
**Toxicity**: Overuse of the product has produced chronic toxicities so applications to large areas for prolonged periods of time are certainly not recommended.
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Mercuric Chloride
**Mercuric Chloride** (HgCL):
Occurs as heavy, white, rhombic prisms, large crystalline masses or
as a white powder
• Odorless
• Soluble in water and alcohol • When the salt is heated, it melts at 277°C to provide a liquid which boils at 300°C, giving off dense white vapors of HgCl Mercuric chloride is sufficiently reactive with proteins to provide anorice solutions are quite utatio when appliedto, the skin and never should be used as an antiseptic for wounds or abraded skin.
**Uses:**
• As a disinfectant solutions (1:1000) for utensils and surgical instruments
• A 1:2000 solution has been employed infrequently as a surgical scrub (handwash).
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Sublime Sulfur
**Sublimed Sulfur N.F. XIII** (Flowers of sulphur)
• It is obtained by condensing the sulphur vapors produced by heating any form of sulphur.
Fine, yellow, crystalline powder having a faint odor and taste. Practically insoluble in water and alcohol and
sparingly soluble in olive oil.
One gram of sublimed sulfur dissolves slowly and usually incompletely in about 2ml of carbon disulfide.
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Precipitated Sulfur
**Precipitated Sulfur U.S.P XVIII (Milk of Sulfur)
• Method of Preparation: Sulfur reacts with boiling solutions of metal hydroxides to form mixtures of metal sulfides and thiosulfates.
For example:
3Са(OH), + 12S — 2 CaS + CaS_03 + 3H20
The products remain in solution but the sulphur can be precipitated by the addition of acid, such as HCl to form
**Precipitated Sulphur U.S.P.**
• with, pale el low, storphous or microcrystalline powder, • Practically insoluble in water, very slightly soluble in alcohol and slightly soluble in olive oil. • Its solubility in carbon disulphide is the same as Sublimed Sulphur.
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Sulfurated Potash
**Sulfurated Potash** N.F. XIII (Liver of sulphur) • Sulfurated Potash N. is a mixture composed chiefly of
potassium polysulfides and potassium thiosulfate. • It contains not less than 12.8% of S (sulphur) in combination
as sulfide. • Occurs as irregular, liver-brown pieces when freshly made,
changing to a greenish yellow colour. • Has an odor of hydrogen sulphide and a bitter, acrid and alkaline taste.
Decomposes on exposure to air.
• Freely soluble in water.
• Alcohol will dissolve only the sulphides. A 1:10 aqueous solution is light brown in colour and alkaline
to litmus.
**Method of Preparation: •** It is prepared by heating potassium carbonate and sulfur to a temperature no higher than 185°C. 185°C
3K,CO3 + 85 -
→ 2K203 + 1202 3 + 300г
When effervescence stops, the heat is increased until perfect fusion results. The melt is cooled by pouring onto a stone slab and converting to protect it from air. The resulting solid is broken into pieces and bottled immediately. The mixture actually consists of potassium polysulfides -
KaS, K_S4, K_S- and K2Sz03.
Uses : • It is official as a pharmaceutical aid as a source of
sulfide.
• It is used in the preparation of White Lotion N.F.
XIII • Used infrequently in lotions and ointments as a parasiticide (scabicide) and in the treatment of acne
and psoriasis.
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Prilocaine
Bupivacaine
Used for Bier’s block
Action lasts 1-2 Hours without adrenaline and double with it
Dose:
6 mg/kg plain
9 mg/kg with adrenaline
Bupovacaine dose - 2 mg/kg
Used for fascia iliaca block
Action lasts - 3-12 hours
129
Selenium sulfide
**Selenium Sulfide N.F. XIII**
• Contains not less than 52% and more than 55.5% of selenium
• Bright orange powder having no more than a faint odor
• Practically insoluble in water and organic solvents
• It is an important nutrient in trace quantities. • In large doses, selenium salts will cause irritation of the gastrointestinal mucosa and damage the renal tubules, spleen anc
bone marrow blood-forming organs. Selenium is not well absorbed through the skin so topical application will not result in selenium toxicity.
**Uses:** Selenium Sulfide is used in shampoos in concentrations of 1 to 2.5% (Selenium Sulfide Detergent Suspension N.F.XIII, Selsun)
as an antiseborrheic.
**Caution:** the preparation should be kept away from the conjuctiva of the eye and prolonged contact with the skin will produce contact dermatitis.
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Cadmium sulfate
**Cadmium Sulfide (Cds)**
• Cadmium is a protein precipitant with a toxicity similar to mercury and greater than zinc. Light yellow or orange colored powder which is
insoluble in water.
**Use** as 1% suspension in the treatment of seborrhea dermatitis of the scalp. It is less irritating than selenium sulfide.
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Astringents
**Astringents are protein precipitants** of limited penetrative power, that is they are able to coagulate protein primarily on the surface of cells, an action that does not result in the death of the cell. • Then the general constriction of tissue e.g. small blood vessels occurs under the influence of astringent.
• The action is mainly topical and lacks deeper effects.
• Astringent compounds have mild antimicrobial actions.
• Astringents are capable of being used safely for their effects on human protein.
Topical astringents are salts of aluminium, zine and to some extent
zirconium.
Note: Compounds used in the previous section can penetrate to the point of tissue damage but astringents don't.
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Uses of astringents
**Uses of astringents**:
• Styptic to stop bleeding from small cuts by promoting coagulation of blood and constricting small capillaries.
• Antiperspirant to decrease secretion of perspiration by constricting pores at the surface of the skin
• Restriction of the supply of blood to the surface of mucous membranes as a means of reducing inflammation
• Direct actions on skin to remove unwanted tissue
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Aluminium chloride
**Aluminium Chloride N.F. XIII**
White or yellowish white, deliquescent, crystalline powder. Nearly odorless Very soluble in water, freely soluble in alcohol and soluble in glycerin •
Acid to litmus in aqueous solutions **Uses:**
local external astringent and mild antiseptic used in aqueous solutions in concentrations ranging from 10 to 25%. Initially employed for use as antiperspirant but was found to be too irritating.
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Aluminium hydroxychloride
**Aluminium Hydroxychloride** (Aluminium Chlorhydroxide)
This name actually applies to two possible compounds: the
monohydroxychloride and
dihydroxychloride [Al(OH), (H20),]+CI- In aqueous solution either one of these will produce a pH higher than aluminium chloride, the dihydroxy compound existing at a higher pH than monohydroxy compound.
• Both the solutions will be acidic.
• It has less water solubility than aluminium chloride.
**Uses** - either one of these compounds or mixtures of the two are used as mild astringents.
Its primary used is as anti-perspirant in concentration of above 20-% and has replaced aluminium chloride.
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Aluminium sulfate
**Aluminium Sulfate** U.S.P XVIII • White, crystalline powder, shining plates or crystalline fragments • Stable in air, odorless, has a sweet taste, becoming mildly astringent
• Freely soluble in water, insoluble in alcohol
• pH of a 1:20 solution should not be less than 2.9 • The compound has chemical properties of aluminium 1or
and sulphate 1on
**Uses: it is a mild astringent** due to presence of aluminium ion. Solutions containing 5 to 25% of the salt are used for their astringent and antiseptic properties. It is recognized officially for the preparation of Aluminium
Subacetate Solution U.S.P
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Aluminium subacetate
**Aluminium Subacetate Solution** U.S.P • It yields from each 100ml not less than 2.3 g and more than 2.6 g of aluminium oxide and not less than 5.43 g and not more than 6.13 g of acetic acid. It may be stabilized by the addition of not more than 0.9%
of boric acid.
**Preparation:**
• Done in class 5. Aluminium Acetate Solution U.S.P XVIII - Done
in class 6. Alum N.F. (Aluminium Ammonium Sulphate or
Aluminium Potassium Sulphate) - Done in class
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Zinc chloride solution
**Zine Chloride U.S.P XVIII**
Uses : • Zinc chloride is used for the activity of zine ion which is a very
strong protein precipitant. The compound is a powerful astringent in solution and mild antiseptic.
The strong astringent properties makes it useful as an escharoti an agent that causes the sloughing of tissue, thus helping in the formation of scar tissue to improve healing). It is applied as a solution containing from 0.5% to 2% of zine chloride. The lower concentration may be applied to mucous membranes and can be used as a nasal spray to aid drainage from infected
sinuses.
• It is applied topically (10% solution) as a desensitizer of dentine.
138
Zinc sulfate
**Zinc Sulphate U.S.P.XVIII**
• Colorless, transparent prisms or as small needles.
• May also be a granular, crystalline powder.
• Odorless, effloresces in air.
• Very soluble in water, freely soluble in glycern and insoluble in alcohol.
• Acid to litmus
**Uses :**
• Used externally as an ophthalmic astringent (Zinc Sulphate Ophthalmic Solution U.S.P.XVIII) in 0.25% aqueous
0.1 ml doses to the conjuctiva.
• Used internally as an emetic (1 to 2 g doses in a 1% solution).
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White Lotion
**White Lotion N.F. XIII**
Preparation : • This is a topical preparation prepared by adding a solution of Sulfurated Potash (40g in 450 ml of water) slowly to a solution of Zinc Sulphate (40g in 450 ml of water) and then adding water to a volume of 1000 ml.
• When completed the resulting product is a suspension of zine sulphides.
K_S + ZnSO - ZnS + K,SO4 • The order of addition of the compounds is very important. If the order is reversed, the hydroxide ions in the Sulfurated Potash cause the formation of basic zine salts and zine hydroxide, rather than zine sulphides. • The precipitate tends to become lumpy upon standing so the suspension should be freshly prepared and shaken thoroughly before using.
**Uses:** • used topically for the effects of sulphide ion and the astringent action of the zine ion. Has been used in the treatment of acne vulgaris, seborrhea dermatitis and
other dermatological problems.
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Toughened Silver nitrate
**Toughened Silver Nitrate** U.S.P XVIII
Properties : • It contains not less than 94.5% of silver nitrate and the
remainder consists of silver chloride (AgCl). • White, crystalline mass generally molded as pencils or
cones. • Breaks with a fibrous fracture, becoming gray or grayish black on exposure to light. • Soluble in water to the extent of its nitrate content always
leaving a residue of silver chloride.
• Partially soluble in alcohol and insoluble in ether.
• Neutral to litmus.
**Preparation:**
• It involves adding hydrochloric acid to a quantity equal to 4% of the weight of the salt, melting the resulting mixture at as low a temperature as possible, and casting in silver molds. • The presence of silver chloride reduces the tendency of the molded product to crumble.
**Uses:** When moistened by dipping in water, toughened silver nitrate can be used to cauterize wounds (coagulate blood and tissue), remove warts and other unwanted growth of
the tissue on the skin e.g granulomatous tissue.
141
Drug’s not adsorbed by **activated Charcoal**
Iron
Lithium
Alkalies
Acids
Alcohols(Ethanol, Methanol, Ethylene glycol)
Organic solvents
142
Rasburicase
Rasburicase is genetically engineered urate oxidase and should be considered for TLS treatment in the presence of high uric acid levels and impaired renal function. Rasburicase enzymatically degrades urate to allantoin. Intravenous administration causes a significant reduction in serum urate concentrations (up to 95%). Rasburicase controls hyperuricaemia faster and more reliably than allopurinol.
143
Lipid soluble Beta blockers
1. Propranolol
2. Carvedilol
3. Labetolol
4. Metoprolol
5. Pindolol
They can cross blood-brain-barrier and can cause - drowsiness, confusion, seizures, hallucinations and coma in overdose.
144
Immunosuppressive drug’s
Azathioprine
Chloroquine
Hydroxychloroquine
Ciclosporin
Cyclophosphamide
Etenercept
Leflunomide
Methotrexate
Mycophenolate mofetil
Penicilamine
Prednisone
Sirolimus
Tacrolimus
Sodium aurothiomalate
145
Digitalis Effect
depressed ST with sagging ST, INVERSE CHECK
Shortened QT interval
T waves: Flat, inverted or biphasic
---------------------------------
**Toxicity Effects**
Marked Bradycardia
Prolonged PR and QRS
Sinus arrest, Varying AV block, paroxysmal atrial tachycardia, escape beats, bigemini, junctional tachycardia
VT, VFib can occur
146
Ethanol
10 ml ie 8 gram is pure one
Calculation of Units: (Total volume of drink x % strength) / 1000
Long term Harm:
- Cardiomyopathy, arrhythmias
- Pancreatitis
- Liver disease, cirrhosis
- UGI bleed
- Gout
147
Tramadol Important Interactions
TCA + Tramadol = risk of seizures
SSRI + Tramadol = risk of seizures
SNRI + Tramadol = risk of seizures
Carbamazepine - reduces Sr Tramadol levels
Warfarin - tramadol increases its effects, INR rises
148
Cyanide antidotes administration
1. **Sodium thiosulfate**:
25 ml of 50% solution over 10 min
2. **Sodium nitrile**:
10 ml of 3% solution over 5-20 min
Measure Meth-Hb if given
3. **Hydroxocobalamin**:
5 grams over 15 minutes iv
4. Dicobalt edetate
300 mg iv over 1 minute immediately followed by 50ml 50% glucose
5. 100% Oxygen, even intubate
149
DigiBind antibody use
**Indications**: digitalis overdose with:
- Hyperkalemia > 6.5, Rx with Glucose/insulin but no calcium iv
- ventricular arrhythmias
- Harmodynamic instability
- Toxicity presents initially as nausea, vomiting, dizziness, yellow vision
**Dose of DigiBind**
No of vials = Digitalis level x weight x 0.01,
Give half first, repeat prn
Rebound rise can occur, monitor 72 Hours
