PharmOrgans Flashcards
(188 cards)
1
Q
CCB MOA and toxicity
A
-blocks voltage depedent L type calcium channels of cardiac and smooth muscle,thereby reducing muscle contractility
-verapamil, diltiazem (heart) > amlodipine, nifedipine (periph)
arteries affected more than veins
Tox: cardiac depression, AVblock, PERIPHERAL EDEMA,FLUSHING, dizziness, constipation, reflex tachycardia,
2
Q
Hydralazine MOA use, toxicity
A
increased cGMP,causing smooth muscle relaxation. Vasodilates arterioles more than veins, decreased afterload
Severe HTN, CHF, first line for pregnany with methyldopa
Tox: compensatory tachycardia, FLUID RETENTION, LUPUS LIKE syndrome
3
Q
Malignant HTN tx
A
nitroprusside, nicardipine, labtolol
4
Q
Nitropruusside MOA/Tox
A
increases cGMP which increases NO, but can cause cyanide toxicity (dilates arteries and vens),
5
Q
HTN drugs used in pregnancy
A
Hydralazine, methyldopa, labetalol, Nifedipine and CCB “HTN moms like Nifedipine”
6
Q
Drugs cauing SLE like sx
A
Sulfonamides, hydralazine, isoniazid, procainamide, phenytoin
7
Q
nitroglycerin, isosorbide, dinitrate MOA,use, tox
A
vasodilates by releasing NO in smooth muscle, causing increased cGMP and smooth muscle relaxation, dilates veins»_space; arteries, causing decreased preload
Use: angina, pulm edema
Tox: reflex tachy, hypoTN, flushing, heaedache
8
Q
HMG-CoA reductase:
- Effect on LDL, HDL, TG
- MOA
- SE/Tox
A
decrease LDL XXX
increase HDL X
decrease TG X
MOA: inhibits HmG CoA to mevalonate
SE: hepatotoxicity,rhabdomyolysis
Check LFTs, CPKs
9
Q
Niacin (VitB3)
- Effect on LDL, HDL, TG
- MOA
- SE/Tox
A
Decrease LDL XX
increased HDL XX
decrease TG X
Inhibits lipolysis in adipose tissue, reduces hepatic VLDL secretion
SE: red flushed face,rash, itching (can decrease overtime or with aspirin use)
hyperglycemia,hyperuricemia
10
Q
Bile acid resins (cholestyramine, colestipol)
- Effect on LDL, HDL, TG
- MOA
- SE/Tox
A
Decreases LDL XX
Increases HDL ~X
Increases TG ~X
Prevents intestinal RAB of BA, liver must use cholesterol to make more
Tox: pts hate it,it tastes bad, GI discomfort, Cholesterol gallstones
11
Q
Cholesteral absorbtion blockers (ezetimibe)
- Effect on LDL, HDL, TG
- MOA
- SE/Tox
A
LDL decreased XX
No HDL change
No TG change
Pevent cholesterol RAB at small intestine at brush border
rarely, rising LFTs and diarrhea
12
Q
Fibrates
- Effect on LDL, HDL, TG
- MOA
- SE/Tox
A
Decrease LDL X
Increase HDL X
Decrease TG XXX
Upregulate LPL, causing increased TG clearance
Mypsitis, hepatotoxic, cholesterol gallstones
13
Q
Cardiac glycosides:
MOA/Use/Toxicity
A
MOA: inhibits Na/K ATPase, leading to indirect inhibtion of Na/Ca exchanger, causing positive inotropy
Use fo CHF (increased contractility), atrial fibrillation (decreased condction at AV node and depresion of SA node)
Tox: cholinergic - nausea, vomitting, diarrhea, blurry YELLOW vision
EKG Changes: increased PR interval, decreased QT interval, T wave inversion, AV block, arrhthmia
can cause hyperkalemia
14
Q
Mg2+ use
A
antiarrythmic - Use for Torsades de pointes and for digoxin toxicity
15
Q
adenoseone use
A
antiarryhthmic which causes increased K efflux, causing hyperpolarization, so no depolarizations allowed
Drug of choice for dx/abolishing SVT
Tox: flushing, hypotension, chest pain
16
Q
Antiarryhthmics - Class 1 MOA
A
Local anesthetic,slow or block conduction, increases effective refractory potential decreaes slope of phase 0, increases thresold for firing in abnormal pacemaker cells
HyperK causes increased toxicity for all class I drugs
Think: Double Quarter Pounder, Mayo Lettuce Tomato, Fries Please
17
Q
Class IA:
Drugs, MOA,Tox
A
quinidine, procainamide,disopyramide
-increases AP duration, increases ERP, increases QT interval
Tox: Qunidine (cinchonism)
procainamide (reversible SLE like syndrome)
disopyramide (heart failure)
thrombocyotopenia, torsades de pointes
18
Q
Class IB: Drugs, MOA,Tox
A
Lidocaine, mexiletine, tocainde
Decreases AP duration, preferentially affect ischemic or depolarized purkine/ventricular tissue
Useful in acute ventricular arrhyhtmias, esecially post MI
Tox: local anestheticcardiovascular depression
19
Q
Class 1C: Drugs, MOA,Tox
A
flecainde, propafenone
MOA: used for ventricular tachcardias that rogress to VF and intractable SVT. Used only as last resort
Tox: proarrythmogenic,especially post mI (CONTRAINDICATED)
Prolons refractory period in AV node
20
Q
Mechanism of action in anti arrythmics and affeceted phase?
A
1: Na blockers - affect p0
2: beta blockers - affect p4
3: potassium blockers - affect p3
4: CCB - affect p0
21
Q
Aniarrhythmics class II Drugs, MOA, tox
A
Metoprolol, propanolol, esmolol, atenolol, timolol
Decrease SA and AV node by decreasing cAMP, decrease Ca currents, decreases slope 4
Tox: impotence,exacerbate asthma, may mask hypoglycemia, can exercbate vasospasm in prinzmetal angina
22
Q
Antiarryhtmics class III
A
amiodarone, Ibutilide, Dofetilide, Sotalol
K channel blockers
Increase AP duration, increase ERP, increased QT interval
Tox:
-sotalol causes torsades de pointes
-Amiodarone: Pulm fibrosis, hepatotoxic,hypo and hyperthyroidism, corneal deposits, photodermatitis, skin deposits
23
Q
Amiodarone toxicity
A
-Amiodarone: Pulm fibrosis, hepatotoxic,hypo and hyperthyroidism, corneal deposits, photodermatitis, skin deposits
Check LFT,TFT,and PFTs for pts on this
24
Q
Class 4 Antiarrythmics
Drugs,MOA, tox
A
Verapamil,diltiazem
MOA:decreases conduction velocity, increases ERP, increases PR interval
Constpation, flushing, edema, torades de pointes
25
Propylthiouracil,methimazole MOA,Use, Toxicity
MOA: block peroxidase, thereby inhibiting organification of iodide and coupling of thyroide hormone synthesis. Also decreases periph converion of T4 to T3
Use: hyperthyroidism
Tox: skin rash, AGRANULOCYTOSIS,aplastic anema, hepatotoxicity
26
Levothyroxine, triiodothyronine MOA,Use, Toxicity
thyroxine replacement,which is used for hypothyroidism
tox: tachycardia,heat intolerance, tremors, arryhtmias
27
GH use?
GH deficiency, Turner syndrome
28
Somatostatin/Octreotride use?
Acromegaly,carcinoid, gastrinoma, glucagonoma (esophaeal varices)
29
Oxytocin
Stimulates labor,uterine contractions, milk let down, controls uterine hemorrhage
30
ADH/desmopressin use?
Central DI
31
Demeclocycline MOA, Use, Toxicity
ADH antagonist
use: SIADH
Nephrogenic DI, photosensitvity, abnl bones and teeth
32
Glucocoticoids
| MOA, Use, Toxicity
MOA: Decrease production of leukotrienes and prostaglandins by inhibting prohpholipase A2 and expression of Cox2
use: addisons, inflammation, immune suppression, asthma
SE: Iatrogenic Cushing's disease - buffalo hump, moon facies, truncal obesity, muscle wasting, thin skin, easy bruiseability, osteoporosis, adrenocortical atrophy, peptic ulcers, diabetes
33
H2 blockers (cimetidine, ranitidine, famotidine, nizatidine) MOA, Use, Toxicity
MOA: reversible block of histamine H2 receptors, causing decreased H+ production by parietal cells
Use: PUD, gastritis, GERD
Tox: Cimetidine inhibits P450, also has anti androgenic effects, can cross BBB (cause confusion,dizziness,and headaches). Cimetidine/ranitidine cause decreased Creatinine excretion by kidneys, thrombocytopenia
34
PPI (omeprazole, lansoprazole, esomeprazole, pantoprazole,dexlansoprazole)
MOA, Use, Toxicity
MOA: Inhibits H/K ATPase i stomach parietal cells
Use: PUD,gastritis, GERD, ZE syndrome, erosive esophagitis
Tox: increased risk for Cdiff infection, pneumonia, hip fractures, decreased serum Mg2+ after chronic use
35
Bismuth/Sucralfate MOA, Use, Toxicity
Binds to ulcer abse, providing protection and allowing HCO3- secretion to restablish pH gradient in mucous layer
36
Misoprostal MOA, Use, Toxicity
MOA: PGE1 analog,increases proxn and secretion of gastric mucous barrier, decreases acid production
Use: prevention of NSAID induced PUD, maintenance of PDA
tox: diarrhea (CONTRAINDICATED IN PREGNANT, causes abortion)
37
Octreotride MOA, Use, Toxicity
Somatostatin analog, used for acue variceal bleeds, VIPoma, carcinoid tumors, acromegaly
Tox: nausea, cramps, steatorrhea
38
Antacid toxicty for AlOH3, MgOH2, and CaCO3
AlOH3: Constipation and hypophosphotemia, prox muscle weakness, seizures, osteodystrophy
MgOH2: Diarrhea, hyporeflexia,hypoTN, cardiac arrest
CaCO3: hypercalcemia, rebound acid secretion
39
Osmotic laxatives (Magnesium hydroxide, magnesium citrate, polethylene glycol, lactulose) MOA, Use, Toxicity
Provide osmotic to draw water out
Use:consntipation (lactulose also for hepatic encephalopathy)
Tox: diarrhea, dehydration
40
Infliximab MOA, Use, Toxicity
Monoclonal Ab to TNFa
used for Chrohns disease, UC, RA
Tox: inffxn (latent TB), fever,hypoTN
41
Sulfasalazine MOA, Use, Toxicity
MOA: combo of antibacterial and anti inflammatory thats activated by gut bacteria
Use; CD, UC (IBD)
Tox: maliase, nausea, oligospermia, sulfonamide toxicity
42
Odansetron MOA, Use, Toxicity
5HT3 antagonist, central anti emetic (okay in pregnancy)
Used for psot op and chemo pts
Headahce, constipation SE
43
Metroclopramide MOA, Use, Toxicity
D2 receptor antagonist, causing increased resting tone, contractility, LES tone, and motility in GI.
use: Diabetic and post surg gastroparesis, antiemetic
Tox: parkinsonian effects,restlessness,drowsiness,fatigue, depression, nauesa, diarrhea
44
Promotility agents (Bethanechol, neostigmine, macrolides, metoclopramide)
MOA for each?
Cholingeric agent: bethanechol, neostigmine
Macrolides (eryhtromycin): increases 5HT
Metoclopramide: decreases dopamine
45
Heparin MOA, Indications, Toxicity
MOA: Cofactor for activation of antithrombin, causes decreased thrombin, decreased factor Xa, short half life
Use: iemdaite anticoag for PE, ACS, MI, DVT, used during pregnancy (safe in pregnancy). Follow PTT
Tox: bleeding, thrombocytopenia (HIT), osteoporsis, drug drug interactions
Note: MWH heparins (enoxaparin, dalteparin) act more on factor Xa and have better bioavailability and 2-4 times longer half life, can be administered subQ without lab monitoring.
46
What is HIT and what is its tx
Development of IgG ab against heparin bound to Platelet Factor 4 - these Ab-heparin-PF4 complexes activate platelets, causing thrombosis and thrombocytopenia
Bivalirudin, lepirudin
47
Lepirudin, bivalirduin?
Derivatives of hirudin, inhibit thrommbin (hence same job as antithrobin), used as alternative to heparin for pts with HIT
48
Warfarin MOA, Indications, Toxicity
MOA: intereferes with synthesis and gamma carboxyltion of Vit K dependent clotting factors II, VII, IX, X and proteins C and S. Does so by inhibiting Vit K epoxide reductase so vit K cannot activate the clotting factors
Metabolized by P450
increased PT/INR
Use: chronic anticoagulation, DVT, PE, Afib)
CONTRAINDICATED IN PREGNANCY
Tox: Bleeding, teratogenic, skin/tissue necrosis, drug-drug interactions
49
Direct Throbin inhibitors?
Argotraban, Dabigatran
50
ThrombolyticsMOA, Indications, Toxicity (tPA/alteplase, streptokinase)
MOA: Aid in conversion of plasminogen to plasmin, which cleaves thrombin and fibrin clots. Increases PT, PTT, but no change in platelets.
Use: early MI, early ischemic stroke, PE
Tox: Bleeding, many contraindications eg pts with active bleeding,intracranial bleeding, surgery, etc...
51
Aspirin MOA, Indications, Toxicity
MOA: Irreversibly inhibits COX1 and COX2 by covalent acetylation. Platelets cannot synthesize newenzymes so effects last until platelets die. Decreased conversion of arachidonic acids to TXA2, increased bleeding time. No change in PT or PTT
Use; Antipyretic, analgesic, anti inflammatory, anti platelet
Tox: Tinnitus (CNVIII), gastic ulceration, ARF< interstinal nepgritis, Respiratory alkalosis, Reye's syndrome
52
ADP receptor inhibitor (clopidogrel, ticagrelor) MOA, Indications, Toxicity
inhibit platelet aggreagation by irrversibly blocking ADP receptors, inhibit fibrinogen binding, prevenging Gp2B3A from binding fibrinogen
Use; ACS, stening, decrease thrombotic stroke
Tox: none really
53
Cilastazol, dipyridamole MOA, Indications, Toxicity
Phosphodiesterase III inhibitor, increases cAMP in platelets, thus inhibiting platelet aggregation, vasodilators
Use: intermittent claudication, coronary vasodilation, prevent stroke/TIA, angina ppx
Tox: Nausea, headache, facial flushing, hypoTn, abdominal pain
54
GpIIbIIIa inhibitors (Abciximabb, tirofiban, eptifibatide)
Bind to Gp2b3a receptor on activatedplatelets, preventing aggregation.
Use: ACS
Tox: Bleeding, thrombocytopenia
55
Direct Xa inhibitors are?
Rivoroxaban, Apixaban
56
LMWH (Enoxaparan, Dalteparin)
Stimulate antithrombin to inactivate Xa, long t/12, subQ injection
57
```
Cancer drugs that work on:
G1 Phase
S Phase
G2 Phase
M phase
```
G1: none
S phase: antimetabolites, etoposide
G2: etoposide, bleomycin
M: vinca alkaloids, taxols
58
Common SE of cancer drugs, and why?
Diarrhea, hair loss, BM supppression --> because these cells are usuaslly rapidly dividing as well and hence are affected
59
Methotrexate MOA, Indications, Toxicity
Folic acid analog that inhibits dihydrofolate reductase --> decrease dTMP --> ddecreased DNA and protein synthesis
ANTIMETABOLITE
Use: leukemia, lymphomas, sarcomas, RA, psoriasis abortion, ectoic pregnancy
Tox: Myelosuppresion (reversible with leucovorin [folinic acid]). Macrovseciular fatty change in liver
Fibrotic lung dz
teratogenic
60
5-fluorouracil MOA, Indications, Toxicity
Pyrimidine analog bioactivated to 5F-dUMP which complexes folic acid --> inibits thymidylate synthase -> causes decreased dTMP --> decreased DNA
ANTIMETABOLITE
USed: Colon cancers, basl carcinomas, pancreatic cancers, ACTINIC KERATOSIS AS TOPICAL USE
Tox: myelosuppresion which is not reversible with leucovorin. OD can be treated with thymidine, uridine
Photosensitivity
61
Cytarabine MOA, Indications, Toxicity
Decreasedpyrimidine analog, which inhibits DNA polyermase
Leukemia/lymphomas
Tox: leukopenia,thrombocytopenia,megalobalstic anemiea
62
Azathioprine/6-MP MOA, Indications, Toxicity
Purine analog --> decreass de no purine synthesis
activated by HGPRT
Works on PRPP amidotransferase
Use: leukemia
Tox: Bone marrow, Gi, liver
Metabolized by xanthine oxidase and thus increased toxicity with allopurinol
63
Dactinomycin MOA, Indications, Toxicity
Intercalates in DNA
WIlms tumor, Eewings Sarcoma, Rhabdosarcoma (PEDIATRIC TUMORS)
Tox: myelosuppression
64
Doxorubin, daunorubicin MOA, Indications, Toxicity
generates free radicals which damage DNA and noncovalently intercaltes in DNA, reaking up DNA
-used for solid tumors, leukemias, and lymphomas
Tox: cardiotoxicity (dilated cardiomyopathy), myelosuppresion, alopecia
Dexrazoxane (used to prevent cardiotox)
65
Bleomycin MOA, Indications, Toxicity
induces free radical formation, which causes breaks in DNA
use in testicular cancer, hodkins lymphoma
PUlm fibrosis, skin changes
66
Cyclophosphamide, ifosfamide MOA, Indications, Toxicity
Covaentlyl X link DNA at guanine. Requires activation by liver
Tox: myelosuppression, HEMORRHAGIC cystitis, partially prevented with mesna, increased risk of TRANSITIONAL CELL CARCINOMA
67
Nitrosoureas (nitrogen mustards) - carmustine, lomustine, semustine MOA, Indications, Toxicity
requrie biactivation, cross blood brain barrier --> CNS
Glioblastoma multiforme, CNS tumors
Cns tox (diziness, ataxia possible)
68
Busulfan MOA, Indications, Toxicity
Alkylates DNA
CML
Tox: Pulm fibrosis,hyperpigmentation
69
Vincristine/Vinblastine MOA/Tox
Alkaloids that bind to tubulin in M phase and block polymerization of microtubules so mitotic spindle cannot form
Tox: vincristine: neurotoxicity (peripheral neuropathy,areflexia)
vinblastine: MYELOSUPPRESSIOn
70
Paclitaxel, taxols MOA/Tox
hyperstabilize polymerized microtubules in M phase so mitotic spindles cannot break down (anaphase cannot occur)
Used in ovarian and brreast carcinomas
Tox: myelosuppression and hypersensitivity
71
Cistplatin, carboplatin, oxaloplatin MOA/Use/Tox
Cross link DNA
Testicular, bladder, ovary, and lung carcinoma
Nephrotoxic,acoustic nerve damage,
Prevent nephrotoxicity with amifostine and chloride diuresis
72
Etoposide,teniposide MOA/Use/Tox
Inhibits topoisomerase II --> causeded DNA degradation
used: SCLC, prostate Ca, testocular cancer
Tox: GI irritation, alopecia, bone marrow suppression
73
Hydroxyurea MOA/Use/Tox
Inhibits ribonucleotide rectuase --> decrease DNA synthesis
Use: melanoma, CML, sickle cell disease
BM suppresison, GI irritability
74
Predisone, prednisolone MOA/Use/Tox
May trigger apoptosis
Tox: cushing like symptoms, immunosuppresion, glaucoma, cataracts, acne, osteoporosis, htn, peptic ulcer disease, hyperglycemia, psychosis
75
Tamoxifen/Raloxifene MOA/Use/Tox
SERMS 0 receptor antagonist in breast and agonists in bone. Blocks binding of estrogen to estrogen receptors.
Used for estrogen + breast cancer tx and prevention. Alsoused to prevent osteoporsis (raloxifene)
Tox:
Tamoxifen: partial endometrial agonist, increases risk fo endometrail cancer
Raloxifene: no endometrail agonist component, no risk
76
Trastuzumab (Herceptin) MOA/Use/Tox
Mab against HER-2, a tyrosne kinase
Her2 positive breast cancer
Cardiotoxic
77
Imatinib (gleevec) MOA/Use/Tox
brc-abl tyrosine kinase inhibitor
Use: CML, GI stromal tumors, ~ALL, ~AML
Tox: fluid retention
78
Rituximab MOA/Use/Tox
Mab against CD20
Use: NHlLymphoma, RA
79
NSAIDs MOA/Use/Tox(Ibuprofen, naproxen, ketorolac, indomethacin)
Reversibly inhibit COX1/COX2, blocks prostaglandin synthesis
Antipyretic, analgesic, anti inflamamtory
Tox: interstitial nephritis, gastric ulcer, renal ischemia
80
Cox-2 inhibitor (celecoxib) MOA/Use/Tox
Reversibly inhibit COX2 found in inflammatory cells and vascular endothelum, which is used for inflammatory and pain, and spares COX-1 which is usually used to maintain the gastric mucosa. Spares platelet fxn as TXA prodx is dependent on Coxx 1
Use: RA, OA, in pts with ulcers and gastrititis
Tox: risk of thrombosis, sulfa allergy
81
Acetaminphen MOA/Use/Tox
Reversibly inhibits cyclooxygenase, mostly in CNS, inactivatedperipherally.
Antipyretic, analgestic,but NOT ANTI INFLAMMATORY. No anti platelet effects. used for children with viral infxn
Tox: OD causes hepatic necrosis
82
Bisphosphonates MOA/Use/Tox
Pyrophosphate analogs, binds hydroxyappatite in bone, inhibits osteoclast activity.
Use: osteoporsis, hypercalcemia, paget's disease of bone
Tox: Corrosive esophagitis, jaw osteonecrosis
83
Allopurinol MOA/Use/Tox
Inhibit Xanthine oxidase, decreases conversion of xanthine to uric acid.
use: Gout, leukemia, lymphoma
Dont give with salicylates.
84
Febuxostat MOA
inhibits xanthine oxidase
85
Probenicid MOA
Inhibits RAB of uric acid in PCT (also inhibits secretion of PCN)
86
Colchicine MOA and SE
Binds and stabilizes ubulin to inhibit polymerization, impaires leukocyte chemotaxis and degradutulation
Tox: GI side effects (diarrhea)
87
Acute gout drugs
NSAIDS (naproxen, indomethacin)
| GLucocorticoids
88
Etanercept MOA use, tox
fusion protein that is a TNFa receptor DECOY
Use: RA, Psoriasis, AS
Tox: CAN CAUSE REACTIVATION OF TB, immunosuppressd via preventing activation of macrophages
89
Infliximan, adalimumab MOA/Use/Tox
Anti TNFa mab
CD, RA,AS,Psoriasis
Tox: reactivate TB
90
Glaucoma drugs MOA
decrease IOP via decreased amount of aqueous humor (inhibit synthesis/secretion or increase drainage)
91
Glaucoma alpha agonists and MOA
epinephrine, brimonine: decrease aqueous humor syntehsis
92
Glaucoma drugs Beta blockers
Timolol, betaxolol, carteolol
| Decrease aqueous humor synthesis
93
Glaucoma drug diuretic
Acetazolamide
| Decreases aqwous humor synthesis via inhibition of carbonic anhydrase
94
Glaucoma cholinergic meds
Pilocarpine, carbachol (direct) and physostigmine (indirect): creases outflow of aqueous humor via contx of ciliary muscle and opening of trabecular meshwork
95
Glaucoma prostagladin drug
Latanoprost, increases outflow of aqueous humor
96
Opiod Analgesics: MOA, use,tox
Morphine, fentanyl,codeine, heroin,methadone, meperidine, dextrometorphan
MOA: Opoid receptor agonists (mu = morphine, delta, kappa) to modulate synaptic transmission. open K+ channels, close Ca2+ channels --> decrease synaptic transmission Inhibits release of ACh, NE, 5HT, glutamate, substance P
Use: pain, cough suppression, diarrhea (loperamide, diphenoxylate), acute Pulm edema
Tox: additiction, resp depression, constpation, miosis, CNS depression
No tolerance to miosis or constipation but does develop to the pain effects
97
Opioid overdose treatment?
Naloxone, naltrexone (opioid receptor antagonist)
98
Tramadol MOA/Use/Tox
Weak opioid agonist, also inhibits 5HT and NE reuptake
use: chronic pain
tox: similar to opioids, decreases seizure threshold
99
Phenytoin MOA/Use/Tox
Increase Na channel inactivation, inhibition of glutamate release fro presynaptic neurons
Use: Tonic clonic seizures
Toxx: GINGIVAL HYPERPLASIA, hirsutism, SJS, Drug induced lupus, induces P450, megaloblastic anemia, osteopenia, peripheral neuropathy
100
Carbamazepine MOA/Use/Tox
increases Na channel inactivation
Use: Simple partial, complexpartial, and generalized tonic clonic seizures , trigeminal neuralgia
Tox: hepatotoxic, Stvens Jonhson syndrome , agranulocytosis, induces P450, SIADH
101
Lamotrigine: MOA/Use/Tox
Blocks voltage gated Na channel inactivation
Use: partial seizures
102
Gabapentin MOA
Designed as GABA analog but primarily inhibits high voltage activated Ca channels,
Use: periph neuropathy, postherpatic neuralgia, migraines, partial and generalized seizures
103
Valproic acid MOA/Use/Tox
Increases Na channel ainactivation, increases GABA concentration
Use: tonic clonic first line, myoclonic seizures
Tox: spna bifida, hepatotoxic, CONTRAINDICAED IN PREGNANCY
104
Ethosuximide MOA/Use/Tox
blocks thalamic T type Ca channels, 1st line for absence seizures
tox: SJS, fatigue, GI heaedache
105
teratogenic epilepsy drugs are...
Phenytoin, carbamazepine, valproic acid
106
Drugs that cause SJS
Ethosuximide, lamotrigine, carbamazepine, phenytoine, phenobarbital
Sulfonamides, penicillins, allopurinol
107
barbiturates MOA/Use/Tox
Facilitate GABA action by increases DURATION of Cl opening
Sedative for anciety,seizures, insomnia, etc..
Tox: cardiorespiratory depression (can be fatal), induces P450
108
BZD MOA/Use/Tox
Facilitate GABA action by increasing FREQUENCY of Cl channel opening.
Tox: dependence,CNS depression
109
Inhaled anesthetic effects/toxicity
Halothane, isoflurane, sevoflurane, nitrous oxide
Myocardial depression, respiratory depression, nausea, increased cerebral blood flow
tox HEPATOXIC (halothane), nephrotoxic (methyoxyflurane), malignant hyperthermia
110
Ketamine MOA
PCP analog that acts as dissociative anesthetic. Blocks NMDA receptors. Cause disorientation, hallucination,and bad dreams
111
Propofol MOA
Used for ICu sediation, rapid anesthetic induction. Potentiates GABA
112
Local Anesthetics MOA/Use/Tox
Esters: procaine, cocaine, tetracaine
Amides: lidocaine, mepivacaine,bupivicaine
MOA: block Na channels by binding to receptor on inner portion of channel. most effective in rapidly firing neurons.
Decreased fxn in decreased pH (like abscess)
Tox: CNS exciation, HTN
bupivicaine: cardiovascular toxicity
cocaine: arrhythmias
113
Succinylcholine MOA, Tox
Depolarizing neuromuscular argent, ACh receptor agonist, produces sustained depolarization and prevents muscle contraction.
Used: muscle paralysis during surgery
Tox: hypercalcemia, hyperkalemia, Malignant hyperthermia (tx with dantrolene)
114
Rocoronium,tobocuranine, mivacirium....
Nondepolarizing neuromusclar blocking drugs, competitive antagonists, comete with Ach for receptors
reversal of blockade with neostigmine, edrophonium, other cholinesterase inhibitors
115
Dantrole MOA/USe
Prevents Ca release from sarcoplasmic reticulum
Use: treat malignant hyperthermia and neuroleptic malignant syndrome
116
Parkinson Drugs
BALSA
| Bromocriptine, Amantidine, L dopa/Carbidopa, Selegiline, Antimuscarincs (eg Benztropine)
117
Bromocriptine, pramipexole, ropinrole
Dopamine agonists (eg used in parkinsons)
118
Amantadine MOA/USE
increases dopamine release
parkinson's disease
119
L dopa/carbidopa MOA/USe/Tox
Dopaminergic agent (converted to dopamine in CNS)
Use in Parkinsons
Tox: arrhythias from increased periph formation of catecholamines. Can lead to dyskinesia after chronic use
120
Selegiline MOA/Use
Selective MA type B inhibtior, helpes prevent L dopa degradation (thus making Dopamine more available)
Use: PD
121
Memantine MOA/Use/Tox
NMDA receptor antagonist, helps prevent excitotoxicity
Use: Alzheimers disease
Tox: dizziness, confusion,hallucinations
122
Donepzil, rivastigmine, galantine MOA/Use/Tox
Acetylcholinesterase inhibitor
Alzheimers
Nausea/dizziness/insomnia
123
Huntingtons drugs
Tetrabanazine,reserpine (inhibit VMAT, limit dopamine release)
Haloperidol (dopamine receptor antagonist)
124
Sumatriptan MOA/Use/Tox
5HT1b1d agonist, inhibits trigeminal nerve activation
use: acute migraine, cluster headaches
tox: coronary vasospasm, CI in prinzmetal/pts with CAD
125
Treatment for alcohol withdrawal
BZD
126
Anxiety tx
SSRI, SNRI, Buspirone
127
ADHD treatment
Methylphenidate, amphettamines
128
Bipolar disorder
Mood stabiizers(lithium, Valproic acid, carbamazepine) , atypical antipsychotics
129
Bulimia tx
SSRI
130
Depression tx
SSRIs, SNRIs, TCAs,buspirone, mirtazapine (esp if they have insomnia)
131
OCD tx
SSRIs, clomipramine
132
Panic disorder
SSRIs, venlafaxine, BZD
133
PTDS
SSRIs
134
Schizophrenia
Antipsychotics
135
Social Phobias
SSRIs
136
Tourettes syndrome
Antipsychotics (haloperidol, risperdal)
137
CNS stimulants: drugs, MOA, use
methylphenidate, dextroamphetatmine, methamphetamine
MOA increases catecholamines at the synaptic cleft, especialyl NE and dopamine.
use: ADHD, narcolepsy, apeptite control
138
Typical Antipsychotics MOA, use, toxicity
Haloperidol, trifluperazine, flupheanzine, thioridazine, chlorpromazine (haloperidol + azines)
All typical antipsychotics block Dopamine D2 receptors (increase cAMP)
Use: schizophrenia (for + sx), psychosis, mania, tourette's syndrom
Tox: slow to remove from body since high lipid solublility, EPS, hyperprolactinoma (from dopamine antagonist), antimuscarinic (dry mouth, constiation), alpha 1 antagonist (hypotension), histamine antagonist (sedation)
Major Tox: NEUROLEPTIC MALIGNANT SYNDROME (rigidity, myoglobinuria, autonomic instability, hyperpyrexia)
TARDIVE DYSKINESIA, NMS especially with haloperidol
139
High and low potency antipsychotics and SE
```
High: Trifluoperazine, flupheanazine, haloperidol
Neurologic SE (EPS) are more common
```
Low: Chlorpromazine,thioridazine - alpha, muscarnicc, histamine side effects
SE: corneal depostis
140
NMS Sx and tx
rigidity, myoglobinuria, autonomic instability, hyperpyrexia
FEVER = Fever, enceophlopathy, vitals unstable, elevated enzymes, rigid muscles
Tx: dantrolene, D2 agonists (bromocriptine)
141
Evolution of EPS side effects Ias sen in antipsychotics/neruoleptics)
4 hr:acute dystonia
4d: akathisisa
4w: bradykiniesiea
4m: tardive dyskinesiea
142
Atipical antipsychotics MOA, use, toxicity
MOA: varied effect on 5HT, dopamine, alpha, and histamine receptors
Clozapine, Olanzapine, quetiapine, risperidone, aripiprazole, ziprasidone
Use: Schizophrenia, positive and negative sx, BPD, OCD< anxiety disorder, depression, mania
Tox: fewer EPS and anticholiernic se than traditional antipsychotics.
Olanzapine/clozapine may cause significant weight gain
Clozapine: AGRANULOCYTOSIS
Ziprasidone: increased QT interval
143
Lithium MOA, use, toxicity
MOA: not established
USe: mood stabilizer for BPD, acute manic events, and SIADH
Tox: tremor, sedation, edema, heart block, HYPOTHYROIDISM, polyuria, teratogenic (ebsteins abnormality), nephrogenic diabetes insipidus
Excreted momstly by kidneys
144
Busprione MOA, use, toxicity
MOA: stimulates 5HT1a receptors
use: GAD, doesnt cause sedation, addiction or tolerance, takes 1-2 weeks for effect.
145
SSRI MOA, use, toxicity
Fluoxetine, paroxteine, sertraline, citalopram
MOA: seratonin specific reuptake inhibitor
Use: Depression, GAD, Panic disorder, OCD, bulimia, socal phobias, PTSD
Tox: GI distress, decreased sexual dysfunction,
seratonin syndrome if combined with other pro seratoningergic drug (MAO, SNRI, TCA) - HYPERTHERMIA, CONFUSION, MYOCLONUS, Cardiovascular collapse, flushing, diarrhea
146
Treatment for seratonin syndrome?
Crpoheptadine
147
SNRIsMOA, use, toxicity
Venlafaxine, duloxetine
MOA: inhibit Seratonin and NE reuptake
use: Depression. ~GAD.panic attacks for velafaxine
Duloxetine also used for pts with diabetic peripheral nueorpathy
tox: increased BP, stimulant effects
148
TCAs MOA, use, toxicity
Amitryptiline, nortriptyline, imipramine, desipramine, clomipramine, doxepin
MOA:Block reuptake of NE and seratonin
Use: major depression, OCD (clomipramine), fibromyalgia
Tox: Tri-Cs - convulsion, coma, cardiotoxicity (arryhtmias) , also respiratory depression,confusion, and hallucinations in elderly due to antcholernigc SE
sedation, alpha 1 blocking effects including hypotension, anticholnergic SE (tachycardia, dry mouth, urinary retention)
Tx: NaHCO3 for cardiovascular toxicity
149
MOA inhibitors: MOA, use, toxicity
tranylcyproamine, phenelzine, Isocarboxazid, elegiline
MOA:: nonselective MAO inhibition, increase levels of amine neurotransmitters (NE, 5HT,dopamine)
Use: atypical depression, anxiety
Tox: Hypertensive crisis (especially with tyramine ingestion) .
Contraindicated with SSRI, TCA, StJohns wort, meperidine, and dextrometoprhan (to avoid Seratonin syndrome)
150
Buproprion MOA, use, toxicity
Increases Ne and dopamine, unsure how
used for depression and smoking cessation
tox: timulant side effects, seizure in bulimic pts, no sexual side effects
151
Mirtazaine MOA, use, toxicity
alpha 2 antagonist (increases release of NE and 5HT and 5HT3 receptor antagonist)
Use: depression, insomnia
Tox: Sedation, increased appetite, weight gain, dry mouth
152
TrazadoneMOA, use, toxicity
MOA: inhibits seratonin reuptake
Use: insomnia mostly
Tox: PRIAPISM, postural hypotension
153
Mannitol MOA, use, toxicity
MOA: osmotic diuretic, increases tublar flow osmolarity, increases urine flow, decreased intracranial and intraocular ppressure
Use: drug OD, elevated intracranial/intraocular pressure
Acute glaucoma, shock
Tox: Pulm edema,dehydration.
Contraindicated in CHF
154
Acetazolamide MOA, use, toxicity
MOA: Carbonic anhydrase inhibitor,which limits NaHCO3 diuresis and reduction in total body HCO3
use: diuresis, glaucoma (decreases prdxn of aqueous humor), **MAINE USE ** --> urinary alkalinzation, metabolic alkalosis, alitutude sickness (to excrete HCO3), pseudotomor cerebri
tox: hyperchoremic metabolic acidosis, sulfa allergy
155
Loop Diuretics MOA, use, toxicity
MOA: sulofamide loop diuretic, inhibits cotransport of Na, K, 2 Cl- of thick ascending limb of loop of Henele. Causes body to lose Ca2+. Prevents urine concentration.
use: CHF, cirrhosis,nephrotic state,hypercalcemia,~HTN
Tox: Ototoxivity, hypokalemia, dehydration, allergy, nephritis, Gout (OH DANG)
156
Thiazides MOA, use, toxicity
chlorthalidone, HCTZ, chlorothiazide
MOA: inhibit NaCl RAB in early dtal tubule, reduces dilating capacity. retains Ca2+ within the body by reducing Ca2+ secretion
Use: HTN, CHF, hypercalcuria, nephrogenic DI
Tox: hyperglycemia, hyperlipidemia, hyperuricemia, hypercalcemia (hyper GLUC)
157
K sparing diuretics MOA, use, toxicity
Spironolactone, triamterne, eplerenone, amiloride
S and E: competitive aldosterone receptor antagonists in collecing tuule
T and A: block Na channels in the CCT
Use: hyperaldosternemia, K+ depletion, CHF
Tox: Hyperkalemia, antiandrogen/progesteronic effects with spironolactone (gynecomastica,menstrual irregularies)
158
Aliskinen
Renin inhibitor, only used in HTN, it is teratogenic
159
ARB: MOA, use, toxicity
Inhibits AII receptors
blocks stimulation of aldosterone
blocks vasoconstriction
no cough, ~angioedemea
160
ACE inhibitors MOA, use, toxicity
Captoppril,lisinopril, enalapril
MOA: inhibits ACE conversion ofAI to AII --> decreases GFR by preventing constrictoin of efferent arterioles. Levels of renin increase. Also, inhibiting ACE also prevents inactivation of bradykinin, a vasodilator.
prevents left heart modeling in HTN,CHF,and postMI pts.
Tox: CATCHH
Cough, angioedema,teratogen, creatinine increase (decrease GFR), hyperkalemia, hypotension
161
Leuprolide: MOA, use, toxicity
GnRH analog with agonist properties if used pulsatile, but antagonist if used continuously (downregulates GnrH receptors in pituitary)
use: infertility (pulsatile),psotate cancer (continuous), uterine fibroids, precocious puerty (continuous)
162
Testosterone, methyltestosterone MOA, use, toxicity
MOA:: agonist at androgen receptors
Use: Treats hypogonadism, promotes development of secondary sex characteristics, stimulation of anabolism to promote recovery afterburn or innjury.
Tox: causes masculinization in females, gonadal atrophy in males, premature closure of epiphyseal plates,increase LDL, decrease HDL
163
Finasteride MOA, use, toxicity
5a reductase inhibitor,which inhibits conversion of testoserone to DHT (more potenet form). Useful in PH and hair growth.
164
Flutamide: MOA, use, toxicity
Nonsteroidal competitive inhibitor of androgens at testosterone receptor, used in prostate carcnoma
165
Estrogens MOA, use, toxicity
bind estrogen receptors
use: hypogonadism in females or ovarian failure, menstrual abnormalities, HRT in postmenopasaul women
tox: increased risk of endometrial cancer, clear cell adenocarcnoma of vagina in females exposed to DES
increased risk of thrombi
CONTRAINDICATIONS: ER positive breast cancer, history of DVTs
166
Clomiphene
SERM: partialagonist at estrogen receptor in hypothalamus, prevents normal feedback inhibiton and increases release of LH and FSH from pituiarty, which stimulates ovulation.
Use: infertility,PCOS
SE: hot flashes, ovarian enlargement, visual disturbances, multiple pregnancies
167
Tamoxifen
Antagonist on breast tissue, used to treat and prevent recurrent ER positive beast cancer
168
Raloxifene
Agonist on bone, reduces resoprtion on bone
169
Hormone Replacement Therapy
Used for relief or prevention of menopausal symptoms and osteoporisis (decreases osteoclast activity)
Upposed estrogen therapy can increased risk for endometrial cancer so progesterone is added too
170
Aramotase inhibitors
Anastrozole, exemestane
used in post menopausal women with breast cancer
171
Progestins use/MOA
MOA: binds progesterone receptors, reduces growth and vascularization of endometrium
Used in OCPs and in treatment of endometrial cancer and abnormal uterine bleeding
172
Mifepristone MOA, use, toxicity
MOA: competitive inhibitor of progestins at progesterone receptor
use: terminate pregnancy
tox: heavy bleeding, GI effects, abnd pain
173
OCPs (dual hormone)
Estrogen and progestins inhibit LH and FSH, and ths prevent estrogen surge,which means no LH surge, which means no ovulation
Progestins: cause thickening of cervical mucus, thereby limiting sperm etnry. Progestins also inhibit endometrial proliferation, decreasing chance of implantation
Contraindicated in smkers > 35 years old (CVD rsk), and datients with history of thromboembolism, stroke
174
Terbutaline
B2 agonist that relaxes the uteris, reduces premature contractions
175
Tamulosin
alpha 1 antagonist used to treat BPH by inhibiting smooth muscle contraction of prostate
176
Sildenafil, vardenefil MOA, use, toxicity
Use: inhibits phsphodiesterase 5, causing increased cGM, smooth muscle relaxation in penis, increases blood flow
Use: ED
Tox: HA, flushing, impaired BLUE GREEN color vision, hypotension
177
Danazol: MOA, use, toxicity
Synthetic androgen that acts as a partial agonist at androgen receptors
Use: endometriosis
tox: weight gain, edema, acne, hirsuitism, masculinzation, hepatotoxicity
178
Asthma drugs include..
Beta 2 agonists, methylxanthines,muscarinic antagonists, corticosteroids, antileukotrienes, omalizumab
179
Muscarininc antagonists
Ipra and tiotroprium - competitive block of muscarinic receptors, preventing bronchoconstriction. also used for COPD.
180
Steroids in asthma use
Beclomethasone, fluticasone: inhibit synthesis of cytokines, inactivate NFkB, the txn factor taht induces prxn of TNFa and other inflammatory agents. 1st line agent ofr chronic asthma
181
zileuton
Antileukotriene - 5 lipoxygenase pathway inhibitor, blocks conversion of arachnidodic acids to leukotrienes
182
Montelukas, zafirlukast
antileukotrienes - blocks leukotriene receptors, especially good for aspirin induced asthama. Blocks LTAD4
183
Omalizumab MOA
monoclonal anti-IgE Ab that binds to serum IgE. used in severe asthma cases
184
Guaifenesin
Expectorant - loosens sputum,thins respiratory secretion, doesnt spress cough reflex
185
N-Acetylcysteine (other than OD)
mucolytic that can loosen mucous plugs in CF patients
can also prevent contrast induced nepropathy
also used for acetaminphen OD
186
Bosentan
Used to treat pulmonary arterial hypertension - antagonizes endothelin 1 receptors, decreases pulm vascular resistance
187
Dextromethophan
Antitussive (antagonizes NMDA glutamate receptors) - synthetic morphine analog
Naloxone can be given for overdose
188
Pseudophedrine, phenylephrine MOA, use, toxicity
Sympathomimetic alpha agonistic nasal decongestants
reduces hyperemia, edema, and congestion, open obstructed eustachian tubes. Pseudophedrine can also be used as a stimulant
tox: HTN, and can cause CNS stimulation, anxiety. Must be careful for medication overdose, causing decreased effects (tachyphylaxis)
