Pharm 101

gsafsaf's version from 2015-05-27 13:29


Question Answer
Full agonistsoccupy receptors to cause maximal activation; intrinsic activity = 1
Partial agonistscan occupy receptors but cannot elicit a maximal response. intrinsic activity = <1
Competitive antagonists Shift the dose-response curve for the agonist to the RIGHT increasing Km; more agonist is required to elicit a response; Vmax unchanged
Noncompetitive antagonistsSame Km; Lower Vmax
Sublingual administrationUseful for drugs with high-first pass metabolism like nitroglycerin, since hepatic metabolism is bypassed
First order velocityVelocity of reaction is directly proportional to the concentration of substrate; the more substrate there is, the faster the reaction occurs
Zero order kineticsReaction velocity is completely independent of substrate concentration; the only way to speed up the reaction would be to add more enzyme so that there are more binding sites for the substrate
First order eliminationConstant FRACTION of drug is eliminated per unit time; most drugs
Zero order eliminationConstant AMOUNT of drug is eliminated per unit time; PEAs are shaped like zeros: Phenytoin, Ethanol, Aspirin
CL(0.7 x Vd)/t1/2
Vd(amount of drug given in IV form)/[drug in plasma]
CL rate of elimination of drug/[drug in plasma]
LD Css x Vd
MDCss x CL
Phase I reactionsHydrolysis, Oxidation, Reduction
Phase I metabolitesSlightly polar, water-soluble, active
Phase II reactionsMethylation, acteylation, glucuronidation, sulfation (conjugation rxns)
Phase II metabolitesNonpolar (do not cross cell membranes readily), inactive, easy to excrete in urine

CYP450 Interactions

Question Answer
CYP450 InhibitorCiprofloxacin
CYP450 InhibitorRitonavir
CYP450 InhibitorAmiodarone
CYP450 InhibitorCimetidine
CYP450 InhibitorKetoconazole
CYP450 InhibitorAcute alcohol use
CYP450 InhibitorMacrolides
CYP450 InhibitorIsoniazid
CYP450 InhibitorGrapefruit juice
CYP450 InhibitorOmeprazole
CYP450 InhibitorSulfonamides
CYP450 InducerGirseofulvin
CYP450 InducerCarbamazepine
CYP450 InducerPhenytoin
CYP450 InducerBarbituates
CYP450 InducerRifampin
CYP450 InducerSt. John's Wort
CYP450 InducerChronic Alcoholism


No effect on CYP450, but Probenicid reduces the excretion of captopril, indomethacin, naproxen, cephalosporins, penicillins, methotrexate, zidovudine, ganciclovir, acyclovir, quinolines, and lorazepam

Common Drug Endings

Question Answer
-afilPhosphodiesterase inhibitor
-caineLocal anesthetics
-cholMuscarinic agonist
-curiumNon-depolarizing neuromuscular blocker
-curoniumNon-depolarizing neuromuscular blocker
-cyclineProtein synthesis inhibitor
-dipineDihydropyridine calcium channel blocker
-fluraneInhaled anesthetics
-gliptinDPP-IV inhibitor (treat DMII)
-glitazoneThiazolidinedione (TZDs; treat DMII)
-mabMonoclonal antibody
-mustineNitrosurea (nitrogen mustard); cross BBB
-navirProtease inhibitor
-prilACE inhibitor
-prostProstaglandin analog
-sartanAngiotensin receptor blocker
-statinHMG-CoA reductase inhibitor
-tidineH2 histamine antagonist
-triptan5-HT agonist
-tropinPituitary hormone

Arachidonic Acid Pathways

Question Answer
Blocks LipoxygenaseZileuton
Blocks Phospholipase A2Corticosteroids
Blocks Cyclooxygenase (COX1+2)NSAIDs
Blocks Cyclooxygenase (COX2)Celecoxib
Blocks Cyclooxygenase (COX2>COX1)Acetaminophen (APAP)
Irreversibly Blocks Cyclooxygenase (COX1>COX2)Aspirin (ASA)
Leukotriene receptor antagonistZafirlukast
Leukotriene receptro antagonist; good for childrenMontelukast
Phosphtidylinositol --> Arachidonic acdPhospholipase A2
Arachidonic acid --> HydroperoxidesLipoxygenase
Neutrophil chemotaxisLeukotriene B4
Increased bronchial toneLeukotrienes
Arachidonic acid --> EndoperoxidesCyclooxygenase (COX1+2)
No anti-inflammatory or anti-platelet effects; Works in CNS to switch off perception of painAcetaminophen (APAP)
Decrease platelet aggregationPGI2
Decrease vascular tonePGI2
Decrease bronchial tonePGI2
Decrease uterine tonePGI2
Increase uterine toneProstaglandins
Decrease vascular toneProstaglandins (E2 + F2A)
Decrease bronchial toneProstaglandins
Increase gastric mucus production Prostaglandins
Increase platelet aggregationThromboxane
Increase vascular toneThromboxane
Increase bronchial toneThromboxane
Only detectible in inflamed tissuesCOX-2

Teratogenic Drugs + Environmental factors

Question Answer
ACE inhibitorsrenal malformations
Fluoroquinolonescartilage damage
Tetracyclinesdiscolored teeth
Cyclophosphamideear/facial anomalies, limb hypoplasia, absence of digits
Methotrexateneural tube defects (folate metabolism), abortion
Carbamazepineneural tube defects (folate metabolism)
Valproic acidneural tube defects (folate metabolism)
Phenytoinfetal hydantioin syndrome (cleft lip, facial/limb abnormalitis, dvlpmtl delay)
LithiumEbstein anomaly - tricuspid valve is displaced downward into RV
StatinsCNS and limb abnormalities
Warfarinfacial/limb/CNS anomalies, spontaneous abortion
IsotretinoinSpontaneous abortion, parathyroid/brain/heart defects; disruption of neural crest cell migration; defective homeobox gene expression
Diethylstilbestrol (DES)clear cell vaginal adenocarcinoma later in life
Thalidomide limb deformity, severe hypoplasia of arms/legs
Alcoholcleft lip/palate, intellectual disability, microcephaly, holoprosencephaly, distinct facial features
CocaineNot exactly teratogenic, but interferes w blood flow to the fetus; restrictive of growth - spontaneous abortion, placental abruption, prematurity
Uncontrolled maternal diabetesNot exactly teratogenic, but assctd w rare condition-caudal regression syndrome (agenesis of sacrum + occasionally lumbar spine, flaccid paralysis of legs, urinary incontinence)
TobaccoNot exactly teratogenic, but interferes w blood flow to the fetus; growth retardation, placental abruption
Vit. A overdoseCraniofacial abnormalities, posterior fossa CNS defects, auditory defects, abnormalities of the great vessels (defects similar to those found in DiGeorge syndrome)

Cardio Side Effects

Question Answer
Coronary VasospasmCocaine
Coronary VasospasmAmphetamines
Coronary VasospasmTriptans
Coronary VasospasmErgotamine
Dilated CardiomyopathyDoxorubicin
Dilated CardiomyopathyDaunorubicin
Torsades de pointes (drugs that increase QT interval)Potassium channel blockers (class III)
Torsades de pointes (drugs that increase QT interval)Sodium channel blockers (class IA)
Torsades de pointes (drugs that increase QT interval)Macrolides
Torsades de pointes (drugs that increase QT interval)Halperidol
Torsades de pointes (drugs that increase QT interval)Chloroquine
Torsades de pointes (drugs that increase QT interval)Protease Inhibitors

Heme Side Effects

Question Answer
Aplastic AnemiaChloramphenicol
Aplastic AnemiaBenzene
Aplastic AnemiaNSAIDs
Aplastic AnemiaPropylthiouracil (PTU)
Aplastic AnemiaMethimazole
Hemolysis in G6PD deficiencyIsoniazid
Hemolysis in G6PD deficiencySulfonamides
Hemolysis in G6PD deficiencyPrimaquine
Hemolysis in G6PD deficiencyAspirin (high-dose)
Hemolysis in G6PD deficiencyIbuprofen
Hemolysis in G6PD deficiencyNitrofurantoin
Hemolysis in G6PD deficiencyDapsone
Hemolysis in G6PD deficiencyFava beans
Hemolysis in G6PD deficiencyNapthalene

GI + Liver Side Effects

Question Answer
Pseudomembranous colitisClindamycin
Pseudomembranous colitisAmoxacillin/ampicillin
Hepatic necrosis Halothane
Hepatic necrosis Acetaminophen
Hepatic necrosis Valproic Acid
Hepatic necrosis Amanita phalloides (mushroom)
Hepatic adenomaOCPs

Systemic Side Effects

Question Answer
Steven-Johnson syndromeCarbamazepine
Steven-Johnson syndromeLamotrigine
Steven-Johnson syndromeAllopurinol
Steven-Johnson syndromePhenytoin
Steven-Johnson syndromePenicillin
Steven-Johnson syndromeEthosuximide
Steven-Johnson syndromeSulfa drugs
Drug-induced lupusSulfonamides
Drug-induced lupusHydralazine
Drug-induced lupusIsoniazid
Drug-induced lupusProcainamide
Drug-induced lupusPhenytoin
Gray baby syndromeChloramphenicol

Endocrine/metabolic Side Effects

Question Answer
Diabetes insipidus Lithium
Diabetes insipidus Demeclocycline
Tertiary adrenal insufficiencyCorticosteroid withdrawal
GynecomastiaAlcohol (chronic use)
Hot FlashesTamoxifen
Hot FlashesClomiphene
GoutDiuretics (loop and thiazide)

CNS/PNS Side Effects

Question Answer
Parkinson-like syndrome Metoclopramide
Parkinson-like syndrome Antipsychotics
Parkinson-like syndrome Reserpine
SeizuresBenzodiazepine/alcohol withdrawal
Tardive dyskinesiaAntipsychotics
Tardive dyskinesiaMetoclopramide
Disulfiram-like reaction Metronidazole
Disulfiram-like reaction Procarbazine
Disulfiram-like reaction First-generation sulfonylureas
Disulfiram-like reaction Disulfiram
Anticholinergic effects Atropine
Anticholinergic effects Tricyclic antidepressants
Anticholinergic effects H1 blockers
Anticholinergic effects Low-potency neuroleptics

Renal Side Effects

Question Answer
Nephrotoxicity + NeurotoxicityAminoglycosides
Nephrotoxicity + NeurotoxicityCisplatin
Nephrotoxicity + NeurotoxicityPolymixins
Nephrotoxicity + Ototoxicity Aminoglycosides
Nephrotoxicity + Ototoxicity Vancomycin
Nephrotoxicity + Ototoxicity Loop diuretics
Nephrotoxicity + Ototoxicity Cisplatin
Hemorrhagic cystitisCyclophosphamide
Hemorrhagic cystitisIfosfamide
Interstitial nephritisNSAIDs
Interstitial nephritisFurosemide
Interstitial nephritisAminoglycosides
Fanconi syndromeTetracycline (expired)

Immunno/Pulm/misc. Side Effects

Question Answer
AgranulocytosisPropylthiouracil (PTU)
FlushingVancomycin (Red Man Syndrome - NOT an allergic reaction)
FlushingDihydropyridine calcium channel blockers
Gingival hyperplasiaPhenytoin
Gingival hyperplasiaVerapamil
Tendinitis/cartilage damageFluoroquinolones
Pulmonary fibrosisAmiodarone
Pulmonary fibrosisBleomycin
Pulmonary fibrosisBusulfan
CoughACE inhibitors


Question Answer
Methamphetamine antidoteAmmonium chloride
Methamphetamine - Rx for SxBenzodiazepines, Antipsychotics, Antihypertensives
Acetaminophen antidoteN-acetylcysteine (replenishes glutathione, which works on elimination + provides sulfhydryl groups to enhance the non-toxic sulfating elimination of the drug)
Salicylates antidote Sodium bicarbonate, dialysis
Organophosphate antidotePralidoxime
Organophosphate - Rx for SxAtropine
Antimuscarinic agent antidotePhysostigmine
ß-blocker antidoteGlucagon, Atropine, Calcium
Non-dihydropyridine Ca2+ channel blocker antidoteGlucagon, Atropine, Calcium
Digitalis antidoteAnti-dig Fab fragments
Digitalis antidoteK+ and Mg++ optimization
Digitalis antidoteAtropine
Iron overload antidoteDeferoxamine
Lead poisoning antidote in childrenDimercaprol, Calcium EDTA, Succimer, Penicillamine
Lead poisoning antidote in adultsCalcium EDTA, Succimer
Mercury, arsenic, gold antidoteDimercaprol, Succimer
Copper, arsenic, gold antidotePencillamine
CO poisoning antidote 100% O2, Hyperbaric O2
Methylhemoglobin antidoteMethylene blue, Vit. C
Cyanide antidoteHydroxocobalamin, Thiosulfate, Nitrates
Methanol antidoteFomepizole, Ethanol, dialysis
Ethylene glycol antidoteFomepizole, Ethanol, dialysis
Opiod antidoteNaloxone (short t1/2), Naltrexone
Benzodiazepine antidoteFlumazenil
TCAs antidoteSodium bicarbonate
Heparin antidoteProtamine
Warfarin antidoteVitamin K (slow), fresh frozen plasma
tPA, streptokinase, urokinase antidoteAminocaproic acid
Theophylline antidoteß-blocker
Tumor Lysis Syndrome "antidote"Allopurinol or Rasburicase

Commonly used disinfectants

Question Answer
AlcoholsDisruption of cell membranes, denaturation of proteins
AlcoholsNOT sporicidal
ChlorhexidineDisruption of cell membranes, coagulation of cytoplasm
ChlorhexidineNOT sporicidal
Hydrogen PeroxideProduces destructive free radicals that oxidize cellular components
Hydrogen PeroxideYES sporicidal
IodineHalogenation of proteins & nucleic acids
IodineYES sporicidal