Drug Classes&Names Flashcards
(217 cards)
1
Q
Bronchodilators (COPD and Asthma Treatment)
A
- beta2 selective agonists
- Leukotriene Inhibitors
- Methylxanthines
- Muscarinic Antagonists
- Antihistamines (mast cell stabilizers)
- Anti-IgE Ab (Omalizumab)
- Corticosteroids
2
Q
Beta2 selective agonists
A
-rol suffix
1. Albuterol (Salbutamol)
2. Terbutaline
3. Fenoterol
4. Salmeterol
5. Formoterol
MOA: Bind β2 Rs on Bronchial tree-> Gs couples Increased cAMP-> Smooth m. relaxation -> Bronchodilation
3
Q
Muscarinic antagonists (for bronchodilation)
A
- Ipratropium
- Tiotropiuum
MOA: M3R inhibitor (Gq-coupled)-> Prevent bronchoconstriction by vagal discharge
4
Q
Methylxanthines
A
Theophylline
MOA: PDE Inhibition-> Increased cAMP-> Bronchodilation, decreased inflammation. CYP450!!
5
Q
Corticosteroids (for bronchodilation)
A
- Budesonide, Dexamethasone
- Prednisolone
MOA: Inhibit PLA2 -> Decrease COX-> Less inflammatory mediators
6
Q
Leukotriene antagonists
A
Montelukast
MOA: Inhibit LT synthesis/action-> Less inflammation + less bronchoconstriction
7
Q
Antihistamines (Mast cell stabilizers - bronchodilation)
A
Cromolyn (not in excel sheet but important)
MOA: Prevent degranulation of mast cells
8
Q
Anti-IgE antibody
A
Omalizumab
MOA: Bind Fc portion of IgE Abs -> cannot bind to mast cells -> no inflammatory response
9
Q
Cough medication
A
- Antitussive agents (non-productive cough)
2. Muco-active (productive cough) - Expectorants& Mucolytics
10
Q
Antitussive agents
A
- Codeine (Opioid)
MOA: μ-Receptor agonist. Suppress cough reflex - Butamirate (Non-opioid) & Prenoxidiazine
MOA: Centrally acting - Suppress cough reflex. Peripheral -> Bronchodilation, suppress inflammation
11
Q
Muco-active Drugs
A
- Mucolytics:
Bromhexine (MOA: Increase serous fluid production)
Acetylcysteine (MOA: Decrease disulfide bonds in mucus, decrease viscosity) - Expectorants
12
Q
Peripheral Vascular Disease drugs
A
- General - Statins, Aspirin/Clopidogrel, Anti-HTN, ACE Inhibitors/ARBs (1st line of treatment)
- Cilostazol (PDE-3 Inhibitor, Vasodilation)
- Pentoxifyllin (Reduce blood viscosity)
- Vinpocetin (Inhibit Na &Ca channels, increase cerebral perfusion)
- Nicergoline (α1 antagonist, Cholinergic function, decrease platelet aggregation, increase metabolism, neurotrophic & antioxidant)
- Ca-Dobesilate (Reduce microvascular permeability)
13
Q
Migraine Treatment
A
- Acute Attack Therapy
2. Prophylactic Therapy (>4 attacks/month, severe attacks, >72hrs)
14
Q
Acute Migraine Attack Therapy
A
- Non-specific:
Acetaminophen, Aspirin, caffeine, NSAIDs, Metoclopramide, Droperidol - Migraine specific:
Sumatriptan (MOA: 5-HT1D/1B agonist, Vasoconstriction, Decreased NP release, brainstem to inhibit pain pathway)
Ergotamine (MOA: Partial 5-HT2& αAR agonist)
15
Q
Migraine Prophylactic Therapy
A
- Galcanezumab (MOA: CGRP antagonist-Vasoconstriction. Minoclonal Ab)
- Cinnarizine (MOA: Anti-histamine, Ca-channel blocker)
- Propanolol (MOA: β-non selective antagonist)
- Verapamil (MOA: Ca-ch. blocker, Non-DHIP)
- Carbamazepin (MOA: Inhibit voltage-gated Na ch, less glutamate release)
- Valproic acid (MOA: Inhibit high-freq. firing, Inhibitory actions of GABA)
- Imipramine (MOA: inhibit 5-HT &NE reupate - Tricylic antidepressant) CYP450!!
16
Q
ACE Inhibitors
A
-pril suffix
1. Captopril
2. Enalapril (1×5-20mg in hypertension)
3. Perindopril
4. Ramipril
MOA: Inhibit ACE, so low AngTensin II and Aldosterone levels, Increase endogenous vasodilators (bradykinin)
First line treatment for Heart Failure
17
Q
ARBs
A
-sartan suffix
1. Losartan
2. Valsartan (1×80-320mg in hypertension)
3. Irbesartan
MOA: Comp inhibitors of AT1R-> Prevent vasoconstriction, low aldosterone, low ADH, decrease SNS stimulation, prevent cardiac hypertrophy
18
Q
Heart Failure Treatment (Decrease load on heart)
A
- ACE Inhibitors/ ARBs
- Diuretics (Thiazides, Loop, K+ Sparing agents)
- Beta blockers
- Vasodilators (isosorbide dinitrate, hydralazine,NO)
- PDE Inhibitors (Milrinone, Theophylline) - For AHF
- Neprilysin inhibitors (Sacubitril) - For CHF
- Ca-sensitizing agents (Levosimendan) - For AHF
19
Q
Heart Failure Treatment (Positive Inotropic agents)
A
Digoxin (maintenance dose 1×0,25mg)
20
Q
Acute Heart Failure Treatment
A
- beta agonists (Dobutamine & Dopamine)
- diuretics (MRAs, Acetazolamide)
- vasodilators (Isoborbide dinitrate, hydralazine)
- PDE Inhibitors (Milrinone, Theophylline)
- ACE Inh/ARBs
- Calcium sensitizers (levosimendan)
21
Q
Chronic Heart Failure Treatment
A
- Digoxin
- Diuretics
- Beta blockers
- ACE-Inhibitors/ARBs
22
Q
Digoxin MOA
A
- Inhibit cardiac Na/K ATPase, Increase Intracellular Na+, Alter driving force for Na/Ca exchanger -> Increased Intracellular Ca -> Increase Ca-release from SR -> Increased actin-myosin interaction -> Increased Contractile force
- Inhibit neuronal Na/K ATPase, Increase Vagal activity-> Negative chronotropy
- Decrease AV conduction -> negative dromotropy
23
Q
Types of Diuretics
A
- Carbonic anhydrase inhibitors
- Osmotic diuretics (aquaretics)
- Loop Diuretics
- Thiazides
- K+ - Sparing
- SGLT-2 antagonists (not used as a diuretic but will increase urine volume)
- Drugs affecting ADH (ADH antagonists)
24
Q
Carbonic Anhydrase Inhibitors
A
Acetazolamide
MOA: Inhibit Carbonic Anhydrase, HCO3- stays in lumen, less H20 reabsorbed in tubule
SOA: Proximal convoluted Tubule
Note: SULFA DRUG (watch for allergies)
25
Osmotic Diuretics (Aquaretic)
Mannitol
MOA: Draws free H20 thus increase Urine Flow
SOA: PCT & Descending loop of henle
CI: HF and Pulmonary edema (due to Mannitol-Induced Extracellular volume expansion)
Glycerol
MOA: Draws free H20. can be metabolized!
Usually used for cerebral edema
26
Loop Diuretics
SOA: TAL
1. Furosemide (20-40mg)
MOA: Inhibit Na+/K+/2Cl- cotransporter. TAL impermeable to water. Loss of volume with a positive potential. SULFA DRUG.
2. Ethacrynic acid
MOA: Inhibit Na+/K+/2Cl- cotransporter but not Sulfa drug. give to Sulfa-sensitive pts
27
Loop Diuretics Side effects & CI
OHH DAANG
Ototoxicity, Hypokalemia, Hyponatremia, Dehydration, Allergy, contraction Alkalosis, Nephritis (interstitial), Gout (hyperuricemia - uric acid crystals).
Ethacrynic acid is more ototoxic
CI: NSAIDs (due to COX-2), Lithium (enhanced effects), Aminoglycoside (otoxicity), Digoxin (electrolyte imbalance)
28
Thiazide diuretics
SOA: DCT
1. Hydrochlorothiazide (in hypertension 6,25-25mg
in congestive heart failure 25-100mg)
2. Indapamide (thiazide-like diuretic) - More for HTN and can combine with ACE inhibitor
MOA: Inhibit Na+/Cl- cotransporter, low diluting nephron capacity, decrease Ca excretion
SULFA DRUGS
29
Thiazide diuretics SE & CI
SE: HyperGLUC
Contraction alkalosis, hyponatremia, hyperGlycemia, hyperLipidemia, hyperUricemia, hyperCalcemia, sulfa allergy
CI: Digoxin (electrolyte imbalances), DM pts (decrease Insulin release by opening K+ channels)
30
K+ - sparing diuretics
1. Aldosterone receptor Inhibitors (MRA): Spironolactone, Eplerone
2. ENaC Inhibitors (Amiloride)
SOA: Collecting duct (principal& intercalated cells)
31
Aldosterone R. Inhibitors Uses
1. Hyperaldosteronism (Conn's Sy)
2. Hypokalemia from other diuretics
3. Congestive HF (inhibits cardiac remodelling)
4. Antiandrogenic use (inhibit 17alpha hydroxylase -PCOS, Female hirutism)
32
ENac Inhibitor Uses
1. Hypokalemia
2. NDI
3. Liddle's sy. (too many ENaCs)
33
Which channels do Aldosterone Receptor Inhibitors affect?
1. Na+/K+ ATPase
2. ENaC
3. K+ channels on apical membrane
4. H+ ATPase (intercalated cell)
34
ADH antagonists (MOA, SOA, SE)
Tolvaptan
MOA: Selective V2R antagonist. ADH cannot bind, no AQP2, promote free water excretion
SOA: Collecting Duct
Use: SIADH & correct hyponatremia
SE: Hypernatremia, Central Pontine Myelinolysis
35
Types of Antiarrhythmic drugs
1. Class I - Na+ channel blockers (Rhythm control)
2. Class II - beta blockers (Rate control)
3. Class III - K+ channel Blockers (Rhythm control)
4. Class IV - Ca channel blockers (Rate control)
5. Class V - Others (adenosine, Mg2+, K+, Digoxin - Rate control)
36
Class I antiarrhythmics
Class IA - Quinidine
Class IB - Lidocaine (preferance for ischemic tissue)
Class IC - Propafenone (CI in pts with ischemic tissue. Proarrhythmogenic effects)
NOTE: Widened QRS complex on ECG
37
Class II antiarrhythmics
beta blockers
1. Cardioselective: Esmolol (IV. acute arrhythmia and intraoperative)
2. Non-selective: Propanolol (Oral. Post-MI to avoid Ventricular Fibrillation)
Note: Can cause Heart Block, presents as prolonged PR interval
38
Class III Antiarrhythmics
MOA: Inhibit K+ channels in phase 2 and phase 3 (thus slowed down. Prolonged refractory period)
1. Amiodarone (Shares properties from Classes I, II, III & IV. Lots of SE)
2. Sotalol (Both a Class III and a beta blocker -> Decrease HR & AV conduction)
NOTE: Can widen QT interval
39
Amiodarone Side Effects
1. Lung fibrosis - Restrictive Lung disease
2. Hepatotoxicity - Hypersensitivity Hepatitis
3. Hypo/Hyperthyroidism
4. Blue/Gray deposits on cornea/skin
5. Photodermatitis
6. AV Block
7. Torsades
8. Inhibit CYP450 so interfere with other CYP450 drugs
9. Induce Heart Failure
40
Class IV Antiarrhythmics
Verapamil
| MOA: Inhibit Ca channels, slow down phase 0 and phase 4 - Rate control + Decrease cardiac contractility and BP
41
Class V Antiarrhythmics
1. Adenosine: A1R activation -> hyperpolarization-> inhibit Ca channels. 1st line agent for acute supraventricular tachys
2. Digoxin: Direct stimulation of vagus nerve
3. K+
4. Mg2+ : can treat torsades and digoxin toxicity
42
Order of treatment for Rate control of AF
1st line: Class II or Class IV
| 2nd line: Digoxin
43
Hypertensive Treatment
Primary HTN: Thiazides, ACE inh/ARBs, DHP Ca Ch. Blockers
HTN with HF: Diuretics, ACE/ARBs, beta blockers (ONLY COMPENSATED HF), MRAs
HTN with DM: ACE/ARBs, Ca ch. blockers, beta blockers
HTN with Asthma: ARBs. Ca ch. blockers, thiazides, selective beta blockers
HTN in pregnancy: Methydopa, nifedipine
44
Types of Antihypertensives
1. Diuretics (Thiazides/ Loop)
2. Sympatholytics
3. Vasodilators
4. RAAS system drugs
45
HTN emergency management
All drugs are given IV.
- Beta blockers (esmolol)
- Ca ch. blockers (Nicardipine)
- Nitroprusside
- Hydralazine
- ACE Inhibitors (captopril)
46
Ca channel Inhibitors
MOA: Inhibit L-Type Ca channels in smooth muscle cells (vessels) and on heart
1. Dihydropyridine (DHP) - more vascular effect
2. Non-dihydropyridines - more cardiac effect
47
DHPs (names, uses, SE)
- Nifedipine: short acting. Do not give in MI or unstable angina pts due to reflex tachycardia. Can give to pregnant women
- Nicardipine: give as IV in HTN emergency
- Felodipine
- Nimodipine
- Amlodipine (long-acting) - 1×5-10mg
Uses:HTN, Raynud syndrome, Prinzmental&Stable angina, Subarachnoid hemorrhage (prevent vasospasm), HTN emergency
SE: Ankle (Peripheral) edema, light-headedness, reflex tachy
48
Non-DHPs (names, uses, SE)
Verapamil
Rate control @ AV&SA nodes (lower HR - Brady), decrease cardiac contractility, decrease myocardial oxygen demand
SE: Constipation, Gingival Hypertrophy, Worsen HF, AV Block if given with beta-blockers, CI in pts with pre-existing heart block
49
Vasodilating drugs for HTN treatment (Not CCB)
1. Nitric Oxide releasing agents (Hydralazine)
2. Endothelin antagonists (Bosentan)
3. PDE-5 Inhibitors (Sildenafil)
50
RAAS pathway drugs as antihypertensives
1. ACE Inhibitors (Captopril, Enalapril, Perindopril, Ramipril)
2. ARBs (Losartan, Valsartan in combo w/ Sacubitril - ARNi, Irbesartan)
3. MRAs (Spironolactone, Eplerenone)
51
Angina pectoris (Ischemic Heart Disease) drug treatment
1. Nitrates (nitroglycerin - 0.5mg sublingual & isosorbide dinitrate)
2. Ca channel blockers (Nifedipine, Verapamil)
3. Beta blockers (Propanolol)
4. Trimetazidine (MOA: partial fatty acid oxidation inhibition - pathway goes into glucose oxidation, less O2 consumption, optimize cellular energy processes)
5. Ivabradine (MOA: Inhibit If Na channels in SA node-> Hyperpolarization-> Lower HR -> Decreased O2 demands)
52
Nitrates SEs and CIs
SE: Headaches, flushing, reflex tachy (prevent with beta blockers), orthostatic HypoTN, methemoglobinemia, tolerance
CI: Systolic BP <90mmHg, Right ventricular MI, Pt taking PDE-5 inhibitors within 24hours, Hypetrophic obstructive cardiomyopathy
53
Dyslipidaemia Drugs
1. Statins
2. Bile acid sequestrants-Resins
3. Sterol absorption inhibitors
4. Fibrates
(not in topic list but 5. Niacin and 6. Others eg Folic acid)
54
Statins
Simvastatin, Atorvastatin, Rosuvastatin (CYP450 DRUGS)
MOA: Inhibit HMG-CoA Reductase, Increase LDL-R Expression (increase cholesterol uptake by liver)
Effect: Highest decrease in LDL, small increase in HDL, small decrease in TGA
Use: CAD pts to increase survival, decrease risk of atherosclerosis & PAD, high risk diabetics
SE: hepatotoxicity, myopathy
CI: Pregnancy, liver disease pts
55
Bile acid sequestrants - resins
Colesevalam
MOA: Bind on bile acids and inhibit absorption in the intestine. Liver uses up its cholesterol to make new bile acids. Lower LDL. Increase LDL-R expression
SE: Constipation, Bloating, Decreased absorption of fat-soluble vitamins (DEAK), Increase VLDL & TGA, Cholesterol gallstones
56
Sterol Absorption Inhibitors
Ezetimibe
MOA: Bind NPC1L1 transporter. Less cholesterol absorption. Liver forced to make own cholesterol. Increase LDL-R Expression. Decrease circulating LDL
SE: Steatorrhea, Increased LFTs
57
Fibrates
Fenofibrate
MOA: PPAR-α agonist. Upregulate LPL -> Hydrolyze VLDL&TGA -> Free fatty acids used up by heart and skeletal muscle for energy
Decrease VLDL & TGA
SE: Cholesterol gallstones, Increased myopathy risk if used with statins
58
Histamine actions
1. Type I allergic rxn (IgE mediated)
2. Increase Vascular permeability
3. Bronchial muscle constriction
4. Increase Nasal&Bronchial mucous production
5. Neurotransmitter (mediate sleep/arousal)
59
Antihistamine drugs
H1R antagonists (1st & 2nd gen)
60
1st generation H1R antagonists
1. Diphenhydramine
2. Promethazine (more sedative/autonomic effects)
3. Dimetindene (less sedative. more allergy txt)
MOA: inhibit central & peripheral H1Rs,Inhibitory effects of alpha1R (dizziness& HypoTN), Musc-R inhibitory effect, serotonin-R inhibitory effects (increase apetite & weight gain). CYP450 DRUGS.
Use: IgE allergies, sedative, antiemetic, sleep-aid, anti-motion sickness, control of nausea&vomiting in pregnancy, manage acute extrapyramidal sxs
SE: Sedation, antimuscarinic effects, Interaction with BZDs&alchohol)
61
2nd generation H1R antagonists
1. Cetirizine
2. Loratadine
3. Fexofenadine
MOA: Inhibit peripheral H1Rs. Do not cross BBB so no autonomic/anti motion sickness effects. CYP450 DRUGS.
Use: IgE med. allergies
SE: Sedation, arrhythmias in overdose, interact with other sedatives
62
Cholinergic Transmission NT and Receptors
NT: Acetylcholine
Receptors: Nicotinic and Muscarinic (Sympathetic and Parasympathetic postganglionic fibers)
63
Cholinomimetics
1. Carbachol (MR &NR) - open angle glaucoma
| 2. Pilocarpine (MR) - closed angle glaucoma, xerostomia
64
Anticholinesterases (Indirect agonists)
MOA: Inhibit Acetylcholinesterase, enhance nAchR activity
Tertiary: Rivastigmine (Alzheimers) & Physostigmine (anticholinergic atropine toxicity - central&peripheral)
Quarternary: Neostigmine (urinary retention, ileus, Myasthenia Gravis, Curare reversal), Edrophonium (MG Tensillon test)
65
Antimuscarinics
MOA: Reversible block. Block Parasympathetic activation
1. Atropine (M3R-Eye & M2R-Heart): mydriasis, increase HR & AV conduction. Dose 0,3-1,0mg
2. Ipratropium, Tiotropium (M3R-Lung): Bronchodilation
3. Oxybutynin, Solifenacin (M3R-Genitourinary): Reduce urinary incontinence
4. Scopolamine(transdermal), Butyl-scopolamine(oral): M1R-CNS, Motion Sickness
5. Cyclopentolate (M3R-Eye): Cycloplegia
6. Procyclidine (M1R-CNS): Parkinson's
66
Catelcholamines
1. Epinephrine (β2&αRs dose dependent) - Anaphylactic shock - sc. or im. 0,15-0,5mg, iv. 0,05-0,1mg
resuscitation 1mg
2. Norepinephrine (α1>α2, β1) - Septic Shock
3. Isoprenaline (β1= β2) - Cardiac arrest, complete heart block
4. Dobutamine (β1> β2) - Cardiogenic shock
5. Dopamine (indirect. D1R, β1 @low dose. D2R @high dose) - increase CNS activity, Increase renal blood flow
67
Indirect sympathomimetics
Ephedrine (Decongestant, HypoTN, stimulant)
MOA: Displace stored catelcholamines from nerve endings
Phenylephrine (HypoTN, Rhinitis, ischemic priapism)
68
Selective α2 agonists
MOA: Bind to α2Rs to decrease sympathetic tone
1. Clonidine - HTN Emergency, Tourette's & ADHD
SE: bradycardia, HypoTN, Decrease CNS action (also binds to I1R)
2. α-Methyldopa - Gestational HTN
SE: Drug-induced lupus
3. Rilmenidine - HTN
SE: milder than Clonidine
Note: Acts on Imidazole R (I1)
4. Oxymetazoline - Decongestant
SE: Only when given systemically, HypoTN
69
α-Receptor antagonists
1. Non-selective : Phentolamine - Pheochromocytoma pre-op, Antidote for HTN due to α-agonist OD
SE: Orthostatic hypoTN
2. α1-selective: Prazosin, Doxazosin, Tamsulosin - HTN, BPH, Prazosin for PTSD
SE: Orthostatic hypoTN
3. α2, α1,β: Urapidil + 5-HT weak agonist - HTN, BPH
4. Both α &β: Carvedilol - HTN Emergency, decrease variceal bleeding, decrease mortality in HF
70
β-Receptor antagonists
1. Non-selective
- Propanolol (Angina, Class II Antiarrhythmic, HTN, thyroid storm, Migraine Prophylaxis, Tremor)
- Timolol (glaucoma)
- Pindolol (HTN in asthma/COPD pts, CI IN HF!!)
- Sotalol (Also a K+ ch antagonist - Class III Antiarrhythmic. SE: Torsades)
2. β1 selective - cardioselective
- Metoprolol ( 2×25-100mg) , Bisoprolol, Nebivolol (HTN, CHF, Angina, Anti-arrhythmics Class II, ACS)
- Esmolol (IV, HTN Emergency, thyroid-storm arrhythmias)
3. β&α combined
- Carvedilol (CHF, Reduce mortality)
71
Centrally acting Skeletal muscle relaxants (Spasmolytics)
1. Baclofen: GABA-b. Cerebral palsy, MS. SE: Sedation, rebound plasticity
2. Diazepam: GABA-a. Chronic&Acute spasm. SE: CNS depressant, tolerance & dependence
3. Tizanidine: α2 agonist. MS, Stroke. SE: sedation, hypoTN, rebound HTN
4. Tolperisone: Na+ & Ca+ ch blocker. Acute spasm. SE: Strong antimuscarinic effects
72
Direct acting muscle relaxants
1. Dentrolene
MOA: RyR1 antagonist -> block Ca+ release in SR -> less actin-myosin interaction
Use: Malignant Hyperthermia. SE: Hepatotoxic
2. Botulinum toxin
MOA: inhibit SNARE to prevent synaptic exocytosis -> Flaccid paralysis
Use: spasm, migraine, cosmetics, hyperhidrosis
73
Skeletal Muscle Relaxants acting on the NMJ
1. Non depolarizing - competitive antagonists at sk muscle nAchRs (Nm) aka. Curare type
2. Depolarizing - agonist at Nm, can stimulate ganglionic nAchR and cardiac M3R
74
Non-depolarizing NMJ anesthetics
1. Mivacurium - short acting. Pseudocholinesterase
2. Rocuronium - IM acting. hepatic metabolism
3. Cisatracurium - IM acting. spontaneous metabolism.
4. Atracurium - IM acting. spontaneous.
5. Piperacurium - long acting. renal metabolism
SE: Histamine release (HypoTN), Prolonged apnea, Tachy
75
Depolarizing NMJ Anesthetics
Succinylcholine (Suxamethonium)
Parenteral with 5-10 min duration. metabolized by cholinesterase enzymes
Use: Surgery with brief duration, Status epilepticus
SE: Arrhythmias, malignant hyperthermia
76
Types of local anesthetics
- Amides
- Esters
Order of nerve blockade: A delta, C, A beta (prefer small, myelinated nerve fibers)
77
Amide local anesthetics
1. Lidocaine (short acting) - CYP450 drug
2. Articaine (short acting, most rapid onset of all LA)
3. Bupivacaine (longest acting, most potent, CNS toxicity, CYP450 drug)
78
Ester Local anesthetics
- Cocaine
| Surface acting, metabolized by pseudocholinesterase, only LA that's vasoconstricting
79
Glucocorticoids (-sone suffix)
| parenteral & oral
1. Hydrocortisone - short acting, replacement therapy in adrenal insufficiency
2. Prednisolone - IM acting
3. Methylprednisolone - IM acting (4-250 mg)
4. Triamcinolone - IM acting. Usually topical. High toxicity compared to others
5. Dexamethasone - Long acting
80
Topical Glucocorticoids
1. Fluocinolone
2. Budesonide
3. Mometasone
4. Fluticasone
81
Mineralocorticoids
1. Aldosterone (endogenous)
| 2. Fludrocortisone
82
Corticosteroid Antagonists
1. MRA antagonists (spironolocatone& eplerone)
| 2. Metyrapone (11 beta hydroxylase inhibition)
83
Androgens
1. Testosterone-undecanoate (testosterone analogue)
2. Nandolon (anabolic steroid)
3. Bicalutamide (Testosterone Receptor Inhibitor)
4. Finasteride (5alpha reductase inhibitor)
5. Goserelin (GnRH analogue)
6. Degarelix (GnRH antagonist)
7. Sildenafil (PDE-5 Inhibitor, Help with Erectile dysfunction)
84
Estrogens and Antiestrogens
1. Ethinyl-estradiol (CYP450 metabolism)
2. Estradiol
3. Tamoxifen (SERM, Hormone-responsive breast cancer)
4. Raloxifen (SERM, Osteoporosis in post-menopausal women)
5. Clomifene (SERM, ovulation induction)
6. Anastrozole (Synthesis Inhibitor-Aromatase, Hormone Responsive breast cancer adjuvant)
7. Goserelin (GnRH analogue, Ovarian suppression, central precocious puberty)
8. Degarelix (GnRh antagonist, Controlled ovarian stimulation)
85
How SERM (Selective Estrogen Receptor Modulators) work
Estrogen antagonist @ breast, CNS, uterus
| Estrogen agonist @liver, bone
86
Progestins
3 types:
1. Pregans - Medroxyprogesterone-acetate, Drospirone, Cyproterone-acetate
2. Estrans - Norethisterone
3. Gonans - Desogestrel, Levonogestrel
MOA: Bing progesterone Rs, decrease growth & increase vascularization of uterus
87
Antiprogestins
1. Mifepristone (Glucocorticoid&Progesteron R antagonist)
Medical abortion in combo with PGE analogue
2. Ulipristal acetate (SPRM)
Day after pill, myoma growth suppression
88
Oral Hormonal Contraceptives
1. Combined: Ethinyl Estradiol + Progestin (Levonorgestrel, Desogestrel, Dosperidone)
2. Minipill (progestin only)
89
Other contraceptives
1. Depot Injection - Medrocyprogesterone-acetate
| 2. IUD -levonorgestrel
90
Thyroid and antithyroid drugs
1. Levothyroxine (T4) - give in hypothyroidism (25-150 µg)
2. Propythiouracil (PTU) - inhibit TPO and 5' deiodinase (hyperthyroidism)
3. Methimazole (Thiamazole) - inhibit TPO
91
How to treat thyroid storm (untreated hyperthyroidism)
1. Beta blockers (propanolol) - treat SNS effects
2. PTU/Methimazole - decrease T3&T4 levels
3. Glucocorticoids (hydrocortisone) - treat opthalmopathy
4. KI
All given IV. PTU & Methimazole given bolus IV
92
Anterior Pituitary Hormone Drugs
GH antagonist:
Octreotide - Inhibit release of GH, Insulin, Glucacon, Gastrin
Prolactin antagonist:
Bromocriptine - D2R agonist, inhibit pituitary secretion of prolactin
93
Posterior Pituitary Hormone Drugs
1. Oxytocin - Oxytocin receptor agonist. Increase uterine contractions & induce labor/ control uterine hemorrhage
2. Desmopressin - ADH agonist (V2R). Treat Nephrogenic DI, Haemophilia A & VWF Disease
94
Anticoagulant drugs types
```
1. Heparin
MOA: Inhibit formation of fibrin clots. Bind ATIII, inhibit factors IX, XI, XII & Plasmin
2. Direct acting thrombin inhibitors
3. Direct acting Factor Xa inhibitors
4. Coumarin - Warfarin
```
95
Heparin drugs
1. Unfractionated heparin (highest chance of HIT. use for DVT, PE, acute MI)
2. Dalteparin - Low molecular weight heparin (watch out for renal insufficiency)
3. Fondaparinux (high specificity to factor Xa)
REVERSE: Protamine Sulfate
96
Direct acting thrombin inhibitors
1. Bivalirudin (anticoagulation in pts with HIT. Give with aspirin during PCI)
2. Dabigatran-etexilate (chronic therapy for AF to prevent clot formation)
97
Direct acting factor Xa inhibitors
Rivaroxiban (prevent venous thromboembolism post-op, prevent stroke in AF)
98
Warfarin uses
CHRONIC anticoagulation (AF, Thrombi, VTE, Post-Mi, heart valve damage)
CYP450 DRUG!
REVERSE: Vitamin K, FFP, PCC
99
Antiplatelet drugs
1. COX inhibitors (Acetylsalicylic acid)
2. Glycoprotein IIb/IIIa Inhibitors (Abciximab)
3. ADP-R antagonists (clopidogrel, prasugrel, ticagrelor)
100
Fibrinolytics (-teplase)
1. Alteplase
2. Reteplase
MOA: tPAs convertin plasminogen into plasmin.
Pernteral.
USE: Acute MI if cannot PCI within 2 hrs. Ischemic stroke. PE (haemo instability), DVT
CI: Cerebral hemorrhage/recent intracranial surgery
SE: Cerebral hemorrhage
101
Bleeding Disorder Drugs
- Vitamin K
Oral/Parenteral
Reverse excessive warfarin anticlotting activity/ Vit K deficiency
- Antiplasmin drugs
MOA: Inhibit plasminogen activation -> No fibrinolysis
1. Aminocaproic acid - Reverse fibrinolysis, use in acute bleeding episodes
CI: DIC, Bleeding of upper urinary tract
SE: Thrombosis, HypoTN, diarrhea
2. Epinephrine
3. Fibrin Foam
102
Anemia drugs
1. Iron - Iron hydroxylide Polymaltose Complex
2. Vitamin B12 (cobalamin)
3. Folic acid (Vitamin B9)
4. Epoetin alpha
5. Filgrastim
103
Parenteral drugs for IDDM
1. Insulin Lispro (Rapid acting)
2. Regular Insulin (short acting)
3. NPH-Insulin (IM acting) - combo w/ short acting
4. Insulin Glargine (long acting)
5. Liraglutide (GLP-1 analogue)
104
Oral antidiabetics
1. Insulin secretagogues:
a) Sulfonylureas (2nd gen - Glimepiride, Glipizide)
b) Meglitines: Repaglinide
2. Biguanides: Metformin (2-3×500-850mg)
3. DPP-4 Inhibitor: Vidagliptin
4. SLGT-2 Inhibitors: Dapagliflozin
5. alpha-glucosidase Inhibitora: Acarbose
105
Agents affecting bone mineral homeostasis
1. Teriparatide - PTH analogue
2. Cholecalciferol - Vitamin D3
3. Raloxifene - SERM
4. Alendronate & Zoledronate - Bisphosphonates
5. Denosumab - IgG Ab
6. Calcitonin
106
1st line treatment in osteoporosis
Bisphosphonates
107
Osteoporosis pharmacotherapy - Inhibit Bone resorption
1. Hormone Replacement therapy
2. SERM
3. Bisphosphonates
4. RANK-L Inhibitors
5. Calcitonin analogues
108
Osteoporosis pharmacotherapy - Increase bone formation
1. Teraparatide
2. Ca2+ supplements
3. vitamin D supplements
4. Thiazides diuretics
109
Autoimmne Disease Drugs
1. Cyclophosphamide (Alkylating agent)
2. Methotrexate (Folate antimetabolite. Inhibit DHF reductase. S-phase)
3. Leflunomide (Inhibit de novo pyrimidine synthesis)
4. Azathioprin (-> 6-MP. Inhibit conversion of PRPP->IMP. No RNA/DNA synthesis. S phase)
5. Mycophenolate - mofetil (IMP dehydrogenase. Less GMP, less WBC proliferation)
110
Cytokine gene expression & 5-ASA derivatives
1. Cyclosporin A (bind cyclophilin, Calcineurin Inhibitor)
2. Tacrolimus- FK506 (Bind FK-binding protein. Calcineurin inhibitor)
3. Sirolimus (mTOR inhibitor)
4. Tofacitinib (Inhibit JAK1&3)
5. Sulfasalazine ( PPAR-γ agonist - Less TLRs&NFkB, Less cytokine, Inhibit COX&LOX. 5-ASA derivative)
111
Antibodies & Fusion Proteins
1. ATG (Bind T-cells. Serum complement destruction)
2. Rituximab (Anti-CD20. Monoclonal Chimeric)
3. Infliximab (Anti-TNFa. Monoclonal Chimeric)
4. Adalizumab (Anti-TNFa. Human)
5. Tocilizumab (Anti-IL6 receptor)
6. Ustekinumab (Anti-IL12&23)
7. Natalizumab (Anti-integrin a4b1. Inhibit WBC entry via BBB)
8. Dupilumab (Anti-IL4 Ra)
9. Abatacept (fusion protein. CTLA-4 fusion protein, Bind CD80/86 on APC)
112
Chemo - Antimetabolites
1. 5-Fluorouracil (Inhibit Thimydilate synthase) - combine with leucovorin for max effect
2. Capecitavine (Bioactivated to 5-FU)
3. Cytarabine (Inhibit DNA polymerase)
4. 6-Mercaptopurine (Inhibit Purine Metabolism)
5. Methotrexate ( Inhibit DHF Reductase)
6. Pemetrexed (Folate antimetabolite)
113
Chemo - Alkylating agents
Interrupt DNA/RNA cross linking
1. Cyclophosphamide (CCNS, Nitrogen mustard)
2. Dacarbazine
3. Temozolamide
4. Bleomycin (Antitumor antibiotic. Free radicals. Pulmonary probs)
5. Dactinomycin (Antitumor antibiotic)
6. Cisplatin & Oxiplatin (inter & intra- strand interruption)
CISPLATIN DOES NOT CAUSE MYELOSUPPRESSION
114
Chemo - Topoisomerase Inhibitors
1. Etoposide (Inhibit Topoisomerase II) - G2 phase
2. Irinotecan (Inhibit Topoisomerase I) - S phase
3. Doxorubicin (antitumor antibiotic. Inhibit Topoisomerase II)
115
Chemo - Mitotic Spindle Inhibition
1. Vincristine (vinca alkaloid, Inhibit MT polymerization)
2. Docetaxel (Inhibit MT degradation so no mitotic spindle formation)
Both M-phase
116
Chemo - Hormonal agents
1. Prednisolone (corticosteroid)
2. Tamoxifen (SERM) - only one given to pre-menopausal women
3. Anastrozole (Aromatase inhibitor)
4. Goserelin (GnRH agonist - continuous)
5. Degareliz (GnRH antagonist)
6. Bicalutamide |(oral non-steroidal antiandrogen)
7. Octreotide (Somatostatin analogue)
117
Chemo - Small molecules
* Tyr-Kinase Inhibitors on Intracellular domain*
1. Imatinib (BCR-ABL t(9;22) )
2. Gefitinib & Erlotinib (EGFR antagonists)
3. Lapatinib (Her2/neu & EGFR antagonist)
4. Sunitinib (VEGFR & PDGFR)
5. Ibrutinib (Bruton's kinase on B-cells)
6. Crizotinib (ALK Kinase & ROS1 oncogene)
7. Bortezamin (Inhibit proteosomal activation of NFkB)
8. Dabrafenib & Trametinib combo (BRAF & MEK - melanoma)
9. Everolimus (Sirolimus derivative, mTOR inhibitor)
10. Tretinoin (Vit A derivative - promyelocyte differentiation)
118
Chemo - large molecules
* Monoclonal Abs. All human except Rituximab*
1. Transtuzumab (Herceptin - AntiHER2/neu)
2. Panitumumab (Anti-EGFR)
3. Rituximab (Anti CD20 - B-cells)
4. Bevacizumab (Anti-VEGF)
5. IFN alpha (antineoplastic, antiviral, immunosuppressant)
6. Aldesleukin (IL-1 recombinant protein)
7. Pembrolizumab (Immunomodulator. PD-1 binding)
119
Opioid analgesics - Natural
1. Morphine - MorphineSO4 oral: 2×30-100mg, Morphine HCL iv: 10-20mg
2. Codeine (anti-tussive)
120
Opioid analgesics - semisynthetic
1. Hydromorphone (analgesia)
2. Oxycodone (abuse)
3. Dihydrocodeine (antitussive)
4. Buprenorphine (withdrawal symptom management)
5. Nalbuphine (spinal anesthesia)
121
Opioid μ analgesics - synthetic
1. Fentanyl (transdermal/sublingual - anesthesia)
2. Tramadol (chronic pain)
3. Meperidine/Pethidine (analgesia in ER)
4. Loperamide & Diphenoxylate (Anti-diarrheals - Loperamide has no CNS effects)
5. Methadone (opioid withdrawal management)
122
Opioid antagonists
1. Naloxone (IV. reverse opioid OD)
| 2. Methyl-naltrexone (Reduce nicotine and alcohol cravings + maintenance)
123
Gout drugs
1. Colchicine (Inhibit MT assembly)
2. Allopurinol (Xanthine Oxidase inhibitor)
3. Rasburicase (Urate oxidase recombinant)
In acute gout attacks, give intraarticular steroids (prednisone)
124
Non-opioid analgesics (NSAIDs)
1. Aspirin (acetylsalicilic acid - irreversible inhibition) dose dependent drug; For inhibiting the platelet aggregation 50-200mg
Analgesic and antipyretic dose 500mg)
2. Ibuprofen (pediatrics) 1-4×200-600mg
3. Indomethacin (Acute gout attack. Closure Ductus Arteriosus)
4. Naloxen (Acute gout. Dysmenorrhea)
5. Diclofenac (MSK pain) 2-3x50mg
6. Metamizole 500-1000mg
7. Ketoprofen (-dex) (lower LTs)
8. Phenylbutazine (Can cause aplastic anemia!)
9. Meloxicam (more inhibition on COX-2)
10. Celecoxib (Cox-2 selective)
11. Acetaminophen (no peripheral COX inhibition)
1-4×500-1000mg
125
Acetaminophen toxicity antidote
N-acetylcysteine
126
Salicylate toxicities (OD)
Tinnitus, abdominal pain, fever, Double acid-base disorder (mixed)
Treat with Activated charcoal and IV NaHCO3
127
Antacids
1. Mg (OH)2
2. Al(OH)3
Decrease Warfarin & Tetracyclines absorption. Increase Quinidine absorption
128
Proton Pump Inhibitors
1. Omeprazole (prodrug. Can inhibit clopidogrel activation)
| 2. Pantoprazole (oral and iv); ORAL: 2×20-40mg
129
H2Receptor inhibitors
Famotidine (decrease NOCTURNAL acid secretion) 2x20mg or 1x40mg
130
Laxatives
1. Senna/ sennoside
2. Bicasodyl
3. Plant fiber
4. MgSO4
5. Lactulose
6. Paraffin oil (pt must be upright when ingesting; avoid Lipoid pneumonia)
131
Antidiarrheals
* μ-opioid agonists in GI*
1. Loperamide (no BBB cross)
2. Diphenoxylate (Must combine with Atropine to avoid CNS effects)
3. Activated charcoal
132
Antiemetics
1. Diphenhydrinate (H1R blocker - combo of diphenhydramine&theophylline)
2. Onsanserton (oral/IV) & Palonoserton (IV) - Inhibit 5HT3Rs in GI
3. Metoclopramide (Inhibit D2Rs. Prokinetic at low dose, Antiemetic at high dose)
4. Dropiredol (Inhibit D2Rs, antipsychotic)
5. Aprepitant (Inhibit NK1R at area postrema) - CYP450 inhibitor
6. Cannabinoid (agonist of CBRs, inhibit presyntaptic DA - AIDS wasting syndrome)
133
Abdominal & Urogenital painkillers /spasmolytics
| smooth muscle drugs
1. Butylscopolamine (Anticholinergic non-selective w/o CNS penetration)
2. Solifenacin & Oxybutynin (M3R inhibitors. transdermal patch)
3. Papaverine (CCB, inhibit PDE. Oral/IV)
134
Tocolytics (Smooth muscle drugs)
1. Atosiban (Oxytocin R antagonist - IV)
2. Terbutaline ( SABA - IV/pos)
3. MgSO4 (IV - also used to prevent seizures in preeclampsia)
4. Ethanol (IV)
135
Uterine contractants (Smooth muscle drugs)
1. Oxytocin (Oxytocin R agonist - IV/intranasal)
2. Ergotamine (Vasoconstrictor- alphaR agonist &partial @ 5TH2, Ergot alkaloid - IV)
NOTE: DO NOT GIVE BEFORE PLACENTA DELIVERY
3. Misoprostol (PGE1 analogue - Oral)
Note: combined with Mifepristone for abortion
136
BPH Smooth muscle drugs
Tamsulosin (uroselective alpha1 blocker - oral)
137
Liver & Biliary tract drugs
1. N-acetylcysteine - acetaminophen toxicity/mucolytic
2. Ursodiol (Decrease cholesterol absorption - CI: Acute hepatitis & biliary obstruction!!)
3. Silimarin (antidote to amanita phalloides - support liver function)
138
Alzheimer's drugs
1. Rivastigmine (Cholinesterase inhibitor, tertiary, cross BBB)
2. Memantine (NMDA-R Blocker)
Nootropic - Piracetam (cognition enhancer)
139
Parkinson's drugs (precursors and endogenous release)
1. Levodopa (DA precursor) - do not give in psychosis
2. Carbidopa (DA DC inhibitor) combined with Levidopa
3. Amantadine (Potentiate endogenous DA & NMDARs inhibitor - less glutamate)
140
Parkinson's - DA R agonists
1. Ropinirole (D2R agonist - non ergot)
| 2. Pramipexole (D3R agonist - non ergot)
141
Parkinson's MAO-I, M1Rs & COMT inhibitor
1. Selegiline (MAO-B inhibitor)
2. Entecapone (COMT inhibitor - peripheral)
3. Procyclidine & Benztropine (inhibit M1Rs - less tremor/dyskinesia)
142
Anticonvulsants - Grand mal txt
1. Valproic acid (Inhibit Na chs, T-type Ca2+ chs, GABA transaminase, Increase K+ permeability in neurons)
2. Phenytoin (Inhibit axonal Na+ chs - does not stop initiation of seizure. Non-linear kinetics)
3. Carbamazepine (Inhibit Na+ chs, no inhibition of initiation
4. Lamotrigine (AMPA-R glutamate antagonist & Inhibit Na+ chs - requires hepatic glucorunidation)
143
Anticonvulsants - Petit mal
1. Ethosuximide (Inhibit T-type Ca2+ chs in thalamus)
2. Clonazepam (BZD - long acting)
3. Valproic acid
144
Anticonvulsants - Myoclonic seizures
1. Clonazepam
2. Lamotrigine
3. Valproic acid
145
Status epilepticus treatment
1. Bolus IV lorazepam/ midazolam/ diazepam
| 2. IV continuous for 5-20' : Phenytoin/ Levetiracetam
146
Anticonvulsants - miscalleneous
1. Vigabitrin (Inhibit GABA transaminase - partial & grand mal)
2. Levetiracetam (SV2AR Block - no glutamate release. Broad spectrum)
3. Phenobarbital (Barbiturate. GABA-A R allosteric binding)
147
Antipsychotics - 1st generation
Phenothiazines: Chlorpromazine (D2R, MRs, alphaR, H1R)
Butyrphenones: Haloperidol (D2R, MR, alphaR) & Droperidol (D2R, H1R)
Thioxanthene: Flupentixol (D2R, 5-HT, alphaR)
148
Antipsychotics - 2nd Generation Atypical (5HT2A Blockade)
1. Clozapine (MAIN: D2R blocker. MR, alphaR, 5HT R block)
2. Olanzapine (5HT, D2R block)
3. Risperidone (5HT R block. No MR block)
4. Aripirazole (PARTIAL D2R & 5HTR agonist)
5. Tiapride (D2/D3 R antagonist)
6. Cariprazine (D2/D3R antagonist - hungarian drug)
149
Bipolar Disorder treatment
1. Lithium (Inhibit Inositol Monophosphatase - Decrease Gq, less Gs action)
Can add Carbamazepine & Valproate
150
Lithium Side Effects
1. Flu-like symptoms
2. GI distress
3. Hypothyroid
4. Nephrogenic DI
5. Acute toxicity
6. Teratogen - Ebstein's anomaly
151
Tricyclic Antidepressants + Tetracyclic and Heterocyclic
1. Clomipramine (TCA - Inhibit NET&SERT)
2. Amitriptyline (TCA - Inhibit NET&SERT)
3. Maprotiline (TetraCA - Inhibit NET more)
4. Bupropion (HeteroCA - Inhibit DAT)
152
Serotonin Antagonist Antidepressants
Trazodone (Post synaptic 5-HT2A Receptor antagonist & SERT)
153
MAO Inhibitors
1. Moclobemide (MAO-A - Antidepressant. Also inhibit Tyramine metabolism. Reversible)
2. Selegiline (MAO-B - Parkinson treatment)
154
SSRIs
* Inhibit presynaptic reuptake of 5-HT*
1. Fluocetine (long T1/2)
2. Citalopram 1x20mg
3. Sertaline
*1st line of treatment for depression & anxiety*
155
SNRIs
* Inhibit NET & SERT. No cholinergic/adrenergic effect*
1. Venlafaxine (Panic, OCD, PTSD)
2. Duloxetine (Diabetic neuropathy)
3. Reboxetine (Selective NET)
156
Atypical antidepressants
1. Mirtazipine (alpha2R selective antagonist - Increase presynaptic release of NE& 5-HT)
2. Agomelatine (MT1R agonist & 5HT2&3R inhibitor)
3. Tianeptine (GABA-R modulator, D2/3 R agonist, 5HT-R inhibitor)
157
Benzodiazepines
*Potentiate GABA by allosterically binding on GABA-A Receptor. Rely on endogenous GABA)
1. Nitrazepam, Midazolam (short acting)
2. Alprazolam (intermediate) 2-3×0,25-0,5mg
3. Diazepam (long acting): 5-10mg
In epileptiform seizures iv. 30mg
4. Clonazepam (long acting)
158
Non-BZD hypnotics
1. Zaleplon (GABAa-R binding)
2. Zolpidem (GABAa-R binding)
3. Melatonin (MT1&MT2 Rs at suprachiasmatic nucleus of hypothalamus) - Sleep ONSET
4. Ramelteon (MT1&MT2 Rs) - sleep ONSET
159
Non-BZD anxiolytics
1. Buspirone (5-HT1 partial agonist)
| 2. SSRIs
160
Barbiturates
* Bind GABAaRs*
1. Thiopental - Short acting, induction of IV anesthesia
2. Phenobarbital - Long acting, Anticonvulsive (oral/IV)
161
IV anesthetics for induction
1. Thiopental
2. Propofol
3. Etomidate (Bind GABAaR)
4. Fentanyl
5. Dexmedetomidine (cental alpha2 agonist - for ICU patients)
162
IV Anesthetics for maintenance
1. Propofol (Potentiate Chloride current via binding GABAaR)
| 2. Fentanyl (opioid μ agonist)
163
Dissociative Anesthesia IV anesthetic
Ketamine (Inhibit NMDA-R complex)
| *CV stimulation*
164
Conscious sedation IV anesthetic
Midazolam (antidote: Flumazenil)
165
IV anesthetics causing CV & respiratory depression
Thiopental, Propofol, Midazolam, Fentanyl
166
Inhaled anesthetics (Gas)
N2O
| >100% MAC value
167
Inhaled anesthetics (volatile liquids)
1. Desflurane (MAC: 6.5%)
2. Isoflurane (1.4%)
3. Sevoflurane (2%)
*NOTE: Skeletal m. hypersensitivity => Malignant hyperthermia. Give Dantrolene*
168
Narrow spectum, beta lactamase SENSITIVE
1. Penicillin G (IV)
2. Penicillin V (oral)
3. Benzathine Penicillin G (IM depot shot)
169
Narrow spectrum, beta lactamase RESISTANT
1. Nafcillin (IV)
2. Oxacillin
* Do not cover MRSA*
170
Broad spectrum, beta lactamase SENSITIVE
1. Ampicillin (IV)
| 2. Amoxicillin (pos) 3×500-1000mg
171
Extended spectrum, beta lactamase SENSITIVE
Piperacillin (IV)
172
Beta lactam combos
1. Amoxicillin/ Clavulanic acid
2. Ampicillin/Sulbactam
3. Piperacillin/Tazobactam
173
Cephalosporins 1st gen
1. Cefazolin (surgical prophylaxis)
2. Cephalexin
*Gram + cocci*
174
Cephalosporins 2nd gen
1. Cefoxitin
2. Cefuroxime
*Gram + cocci with gram - coverage*
175
Cephalosporins 3rd gen
1. Ceftriaxone (hospital acquired pneumonia & single IM dose for gonorrhea)
2. Cefotaxime
3. Cefixime
4. Ceftazidime (pseudomonas)
*Gram - increased coverage*
176
Cephalosporins 4th gen
Cefepime (broad spectrum, beta lactamase resistant)
*Pseudomonas!*
177
Cephalosporins 5th gen
1. Ceftaroline fosamil
2. Ceftalozane/tazobactam
*TREAT MRSA!*
178
Probenecid inhibits tubular secretion of _____
1. Cephalosporins
2. Penicillin
3. Methotrexate
179
Monobactam
Aztreonam
MOA: Bind PBP-3 ONLY in Gram- bacteria
(Klebsiella, Pseudo, Serratia)
180
Carbapenems (2nd gen)
1. Imipenem (decrease seizure threshold)
2. Meropenem
*Reserve Antibiotics, Pseudomonas. Resistant to most beta lactamases
181
Glycopeptide Antibiotics
MOA: Bind D-Ala-D-Ala, inhibit transglycosylation. BACTERICIDAL. Parenteral
1. Vancomycin
2. Teicoplanin
3. Ortivancin
182
Lipopeptide antibiotics
MOA: Irreversibly inserts into cytoplasmic membrane, disrupt gradient. BACTERICIDAL
Daptomycin (MRSA, VRSA, VRE)
*NOTE: causes rhabdomyolysis, be careful if patient takes statins too*
183
Polypeptide Antibiotics
MOA: Inhibit peptidoglycan precursos translocation. Bactericidal/ Bacteriostatic
Bacitracin (topical due to severe nephrotoxicity)
184
Tetracyclines
MOA: Bind 30S. Bacteriostatic. Chelators (Ca, Fe, Mg). Accumulate in teeth - teratogen
1. Tetracycline (pos)
2. Doxycycline: first day 200 mg, than 100 mg 1x daily
3. Tigecycline (IV only) - Glycylcycline
185
Aminoglycosides
MOA: Bind 30S, Needs O2 to penetrate cell wall (combine with beta lactams). Inhibit initiation complex, induces misreading of mRNA & inhibit translocation => Bactericidal
1. Gentamycin - Tobramycin -Amikacin -Netilmicin
2. Streptomycin (combine with penicillin)
3. Neomycin - Kanamycin (Topical. Orally- remains active in GI tract)
186
Chloramphenicol
MOA: Reversible binding of 50S. Bacteriostatic
Used as a topical treatment due to toxicity
Empirical treatment of bacterial meningitis
CYP450 Inhibitor. Suppress RBC production. Grey baby syndrome
187
Oxazolidones
Linezolid
MOA: Bind 50S. Inhibit initiation complex for translation. Bacteriostatic
Inhibit MAO-A & B
MRSA, PRSP, VRE
188
Macrolides
MOA: Bind 50S. Bacteriostatic
1. Erythromycin (txt walking pneumonia). Inhibit CYP450
2. Roxithomycin (no activity against MRSA & PRSP). Inhibit CYP450
3. Azithromycin 1x500mg for 3 days
4. Clarithromycin. CYP450 Inhibitor
189
Ketolides
MOA: Similar to macrolides, especially erithromycin
Telithromycin (use for macrolide-resistant strains. CYP450 Inhibitor)
190
Clindamycin
MOA: Bind 50S. Bacteriostatic
Narrow spectrum. For Gram+ due to poor penetration of Gram - outer membrane.
NOTE: Can have C.difficile superinfection!
191
Streptogramin
MOA: Bind 50S - block exit channel on ribosome. Bactericidal
1. Quinupristin
2. Dalfopristin
*Reserve antibiotics. CYP450 Inhibitor*
192
Antimetabolite (antifolate) antibiotics
1. Sulfonamides (Inhibit DHP synthase)
2. Trimethoprim (DHF reductase inhibitor)
3. Pyrimethamine/Sulfadiazine (Txt for toxoplasmosis)
4. Proguanil (malaria prophylaxis)
*TMP-SMX combo is bactericidal*
193
Fluoroquinolones (-floxacin)
MOA: Inhibit DNA gyrase (topoisomerase II) in Gram - and Topoisomerase IV in Gram+
Bactericidal. Post Antibiotic effect
1. Norfloxacin/ Ciprofloxacin/ Ofloxacin (2nd gen)
2. Levofloxacin (3rd gen) - Respiratory walking pneumonia
3. Moxifloxacin (4th gen)
194
Metronidazole
MOA: Forms free radicals
Bacteridical. High CSF concentration
CYP450 Inhibitor
Also used to treat protozoal diseases
195
Fidaxomicin
MOA: Inhibit bacterial RNA pol. Oral
Bacteridical
Can txt C.difficile
196
Rifaximin
MOA: Inhibit DNA-dep RNA pol
Rifampicin derivative
*Use in Hepatic encephalopathy*
197
Mupirocin
MOA: Inhibit bacterial protein synthesis by binding isoleucyl tRNA synthetase
Topical (not absorbed)
198
Fusidic acid
MOA: Inhibit bacterial elongation factor G
Bacteriostatic
Topical for skin infections & Oral for MRSA
199
Polymyxin E
MOA: cationic detergent. Bactericidal
200
Fosfomycin
MOA: Inhibit enolpyruvate transferase -> No N-acetylglucosamine (cell wall precursor)
Bactericidal
201
Nitrofurantoin
Urinary antiseptic
| No systemic antibacterial effects
202
TB 1st line treatment
1. Isoniazid (inhibit mycolic acid synthesis-Bactericidal -CYP450 Inhibitor)
2. Rifampin (Inhibit DNA-dep. RNA pol - Bactericidal)
3. Ethambutol (cell-wall synthesis inhibitor)
4. Pyrazinamide (no known MOA. bacteriostatic)
RIPE - Phase I: 2 months
Phase II: 4-7 mo. Rifampin & Isoniazid
203
TB 2nd line
1. Streptomycin/ Amikacin/ Kanamycin
| 2. Cycloserine (inhibit peptidoglycan synthesis)
204
Leprosy treatment
1. Dapsone ( Inhibit folic acid synthesis - Bacteriostatic)
| 2. Rifampin
205
Antiherpetic agents
1. Acyclovir (Inhibit viral DNA pol - HSV1/2, VZV & IV for HSV encephalitis)
2. Valaciclovir/Famciclovir (Inhibit viral DNA pol - VZV & acyclovir resistant strains)
3. Ganciclovir (Inhibit viral DNA pol - 1st line for CMV)
4. Valganciclovir (ganciclovir prodrug with better oral bioavailability)
5. Cidofovir (Inhibit Viral DNA pol - HSV, CMV, HPV, Adenovirus & TK- strains. IV)
6. Foscarnet (not an antimetabolite - Inhibit both RNA&DNA pol - CMV 2nd line agent. IV)
206
Antiretrovirals - NRTIs
MOA: Prodrugs. Inhibit binding of nucleosides to reverse transcriptase
1. Zidovudine - Pregnancy safe
2. Lamivudine - also used for Hep B
3. Emtricitabine - CI in pregnancy/child/ renal&hepatic Failure
4. Abacavir
5. Tenofovir - also used for Hep B. No phosphorylation needed for activation
6. Stavudine (do not use with zidovudine)
7. Didanosine - dose dependent pancreatitis
8. Zalcitabine
207
Antiretrovirals - NNRTIs
MOA: Bind on reverser transcriptase (diff site from NRTIs). No phosphorylation needed.
Not active against HIV-2
1. Etravirine (Inhibitor + Inducer of CYP450)
2. Nevirapine (CYP450 Inducer) - Used to prevent vertical transmission
3. Efavirenz (TERATOGENIC)
4. Delavirdine (Teratogenic)
208
Antiretrovirals - Protease Inhibitors, Integrase inhibitors & entry inhibitors
1. Maraviroc (Blocks CCR5 receptor so no interaction b/w viral gp120 and CD4 on lymphocytes)
2. Elvitegravir (Bind integrase so viral DNA cannot integrate in host DNA)
3. Ritonavir (PI - most common. MOST POTENT CYP450 INHIBITOR)
4. Lopinavir (PI - use with ritonavir)
NOTE: Ritonavir is often added to HIV txt to increase serum levels of other antivirals due to CYP450 inhibition
209
Anti-influenza
1. Amantadine/ Rimantidine (Inhibit M2 protein needed for onset of infection)
2. Oseltamivir/ Zanamivir (inhibit neuramidase - no new virion clumping)
210
Anti-RSV
1. Palivizumab (Human monoclonal Ab - no fusion)
| 2. Ribavirin
211
Hepatitis antivirals (non specific)
1. IFN-α (activate cytokines, increase JAK-STAT path)
2. Entecavir (guanosine analogue - Inhibit HBV DNA pol)
3. Tenofovir (NRTI)
4. Ribavirin ( Guanosine analogue, Inhibit IMP DH so no GMP. No Viral RNA pol)
212
Uses of IFN-α
Hep B, HHV-8, Hairy cell leukemia, malignant melanoma, papillomatosis, RCC, HPV
213
Hepatitis antivirals (DAAs)
1. Paritaprevir/ Grazoprevir (PI - NS3/4A)
2. Sofosbuvir (NPI - NS5B)
3. Dasabuvir (NNPI - NS5B)
4. Velpatasvir/ Elbasvir (NS5A)
214
Malaria drugs
1. Chloroquine (Inhibit heme polymerization) + Hydroxychloroquine (less toxic and for AI)
2. Mefloquine (Unknown MOA - blood schizontocide)
3. Quinine (Inhibit protozoal DNA replication - schizontocide)
4. Artemether (Produce free radicals - schizontocide)
5. Lumefantrine (Unknown MOA)
6. Malarone= Proguanil (Inhibit DHFR Thimydylate synthase) + Atovaquone (disrupt mitochondrial metabolism)
7. Primaquine (Tissue schizonticide - oxidants)
215
Helminthic infections
1. Mebendazole (Inhibit MT synthesis & glucose uptake)
2. Ivermectin (Facilitate GABA-med. transmission thus immobilized parasites due to hyperpolarization)
3. Niclosamide (Uncouple oxidative phosphorylation)
216
Antifungal agents
1. Amphotericin B (Form pores in fungal membrane by interacting w/ ergosterol. Fungicidal)
2. Nystatin (same as amphotericin but only TOPICAL due to toxicity)
3. Clotrimazole (Imidazole. Topical, OTC. Interfere with ergosterol synthesis. CYP450 Inhibitor)
4. Fluconazole (1st gen Triazole. Cross BBB so can txt Cryptococcus meningitidis. Interfere w/ ergosterol synthesis. CYP450 Inhibitor)
5. Itraconazole ( 1st gen Triazole. CYP450 Inhibitor)
6. Voriconazole (2nd gen Triazole, for Aspergillus. Cause Visual disturbances. CYP450 Inhibitor.)
7. Flucytosine (5-FU, Incorporate into fungal RNA & Inhibit thimidylate synthase. Antimetabolite)
8. Caspofungin (Echinocandin. Inhibit synthesis of beta(1,3) glucan of fungal cell wall
9. Terbinafine (Inhibit squalene epoxidase - fungal membrane)
217
Disinfectants & Antiseptics
Alcohols: Ethanol 70%, Isopropyl alcohol 70-90%
Halogens: Povidone-iodine
Oxidizing agents: H202
Chlorinated phenols: Chlorhexidine
Cationic surfactant: Octenidin, Invert soaps
