Pharmacology Flashcards
Km =
[S] at 1/2 Vmax
Lineweaver Burk plot formula
1/V = (Km/Vmax)(1/[S]) + 1/Vmax
A higher Y intercept on a lineweaver Burk plot means
lower vmax
the X intercept of a lineweaver burk plot is
-1/Km. Closer to zero = lower affinity
A high Km means
low affinity
Vd =
(amount of drug in body) / (plasma concentration)
CL =
Vd * Ke
number of half lives to reach 90% steady state
3.3 (first order only)
number of half lives to reach steady state
4-5 (first order only)
T 1/2 =
0.693 Vd/CL (first order)
Loading dose =
(1/F)(Cp*Vd)
Maintenance dose =
(1/F)(CpCLtime interval)
Drugs with zero-order kinetics
PEA: phenytoin, ethanol, aspirin (at high or toxic concentrations)
These are part of sympathetic system but innervated by cholinergic fibers
adrenal medulla (nicotinic) and sweat glands (muscarinic)
these are innervated by Nn (nicotinic) nerves
parasympathetic ganglia, adrenal medulla
these are innervated by Nm (nicotinic) nerves
NMJ
alpha 1 (G, function)
Gq. vascular contraction, close bladder, close GI sphincters, dilate eyes
alpha 2 (G, function)
Gi. reduced symp outflow, decrease insulin, decrease lipolysis, decrease aqueous humor production, increase platelet aggregation
beta 1 (G, function)
Gs. stimulate heart, renin, lipolysis
beta 2 (G, function)
Gs. vasodilate, bronchodilate, increase lipolysis and insulin release, increase aqueous humor, decrease uterine tone, relax ciliary muscle
beta 3 (G, function)
Gs. lipolysis, thermogenesis in SKM
M1 (G, function)
Gq. CNS, enteric
M2 (G, function)
Gi. antagonize heart
M3 (G, function)
Gq. exocrine glands/gut, contract bladder, bronchoconstriction, constrict eyes, contract ciliar muscle (accomodation)
D1 (G, function)
Gs. relax renal vasculature
D2 (G, function)
Gi. neurotransmitters
H1 (G, function)
Gq. mucus, permeability, bronchoconstriction, pruritus, pain
H2 (G, function)
Gs. gastric acid secretion
V1 (G, function)
Gq. vascular smooth muscle contraction
V2 (G, function)
Gs. increases H2O permeability in collecting tubules of kidney. “V2 found in the 2 kidneys”
Gq acts via this/these pathway(s)
Phospholipase C –> DAG and IP3
DAG –> protein kinase C
IP3 increases intracellular calcium
these GPCRs use Gq
H1, A1, V1, M1, M3 (HAVe1 M&M)
these GPCRs use Gi
M2, A2, D2 (MAD 2s)
Gs/i act via this/these pathway(s)
stimulate or inhibit adenylyl cyclase.
Adenylyl cyclase increases cAMP —> protein kinase A –> heart contraction, but muscle relaxation elsewhere
this drug blocks choline entry
hemicholinium
this drug blocks ACh incorporation into vesicles
vesamicol
this drug blocks ACh vesicle fusion/NT release
botulinum
this drug blocks tyrosine conversion to DOPA
metyrosine
this drug blocks dopamine incorporation into vesicles
reserpine
this drug prevents nore release
bretylium or guanethidine
this drug displaces NE in vesicles and reverses the NET transporter
amphetamines
indirect choline agonists used for Alzheimer disease
donepezil, galantamine, rivastigmine
this is a tertiary amine anticholinergic that crosses the BBB
pysostigmine
antispasmodics for IBS
hyoscyamine, dicyclomine (anti-muscarinic)
class of drugs for oxybutynin, solifenacin, tolterodine
muscarinic antagonists
tropicamide is similar to
atropine
albuterol, salmeterol specificity
B2 > B1
dobutamine specificity
B1 > B2, a
dopamine specificity
D1 = D2 > B > a
epi specificity
B > a
nore specificity
a1 > a2 > B1
fenoldopam specificity
D1
Isoproteronol specificity
B1 = B2
midodrine specificity
a1
phenylephrine specificity
a1 > a2
this drug increases NE release (not amphetamines)
ephedrine
guanfacine is similar to
clonidine
alpha-methyldopa class and application
alpha-2 agonist, used to treat hypertension in pregnancy
which adrenergic drugs treat open angle glaucoma by reducing aqueous humors
epi (via a2) and beta blockers
which drugs exacerbate closed angle glaucoma
dilators of the eye, including atropine (muscarinic blocker)
this drug is contraindicated in cocaine intoxication
beta blockers
antidote/tx for acetominophen
n-acetylcysteine (replenishes glutathione)
antidote/tx for benzos
flumazenil
antidote/tx for copper
penicillamine, trientine
antidote/tx for cyanide
nitrite + thiosulfate, hydroxocobalamin
antidote/tx for heparin
protamine sulfate
antidote/tx for iron
deferoxamine, deferasirox, deferiprone
antidote/tx for arsenic or mercury
dimercaprol, succimer
antidote/tx for gold
penicillamine, dimercaprol, succimer
antidote/tx for lead
EDTA, penicillamine, dimercaprol, succimer
antidote/tx for methanol, ethylene glycol
fomepizole (alc dh blocker) > ethanol, dialysis
antidote/tx for methemoglobin
methylene blue, vitamin C
antidote/tx for salicylate and TCAs
they’re acidic, so use sodium bicarbonate. could also use dialysis for salicylates
antidote/tx for amphetamines
they’re basic so use NH4Cl to acidify urine
drugs that cause cutaneous flushing
vancomycin, adenosine, niacin, CCBs, echinocandins (VANCE)
this drug prevents doxorubicin-induced cardiomyopathy
dexrazoxane
these drugs cause hyperglycemia
tacrolimus, protease inhibitors, niacin, HCTZ, corticosteroids
(“Taking pills Necessitates Having blood Checked”)
these drugs cause focal to massive hepatic necrosis
halothane, amanita phalloides, valproic acid, acetaminophen (liver “HAVAc”)
these drugs cause hepatitis
rifampin, isoniazid, pyrazinamide, statins, fibrates
these drugs cause pancreatitis
didanosine, corticosteroids, alcohol, valproic acid, azathioprine, diuretics (furosemid, HCTZ)
(“Drugs Causing A Violent Abdominal Distress”)
these drugs cause pill-induced esophagitis
tetracyclines, bisphosphonates, potassium chloride
these drugs cause agranulocytosis
clozapine, carbamazepine, propylthiouracil, methimazole, colchicine, ganciclovir
“Can Cause Pretty Major Collapse of Granulocytes”)
these drugs cause aplastic anemia
carbamazepine, methimazole, NSAIDs, benzene, chloramphenicol, propylthiouracil
(“Can’t Make New Blood Cells Properly”)
these drugs cause direct coombs-postive hemolytic anemia
methyldopa, penicillin
this drug causes gray baby syndrome
chloramphenicol
these drugs cause hemolysis in G6PD deficiency
isoniazid, sulfonamides, dapsone, primaquine, aspirin, ibuprofen, nitrofurantoin
(hemolysis “IS D PAIN”, note also naphthalene (moth balls) and fava beans in med. type)
these drugs cause megaloblastic anemia
phenytoin, methotrexate, sulfa drugs (“having a blast with PMS”)
these drugs cause fat redistribution
protease inhibitors, glucocorticoids (“Fat PiG”)
these drugs cause gingival hyperplasia
phenytoin, CCBs, cyclosporine (but not tacrolimus)
these drugs cause hyperuricemia
pyrazinamide, thiazides, furosemide, niacin, cyclosporine (“Painful Tophi and Feet Need Care”)
these drugs cause osteoporosis
steroids, heparin
these drugs cause photosensitivity
sulfonamides, amiodarone, tetracyclines, 5FU
“SAT For Photo”
these drugs cause Stevens-Johnson
anti-epileptics (especially lamotrigine), allopurinol, sulfa drugs, penicillin
these drugs cause teeth discoloration
tetracyclines
these drugs cause tendonitis, tendon rupture, and cartilage damage
FQs
these drugs cause a Parkinson-like syndrome
antipsychotics, reserpine, metoclopramide
“cogwheel ridigitidy of the ARM”
these drugs cause seizures
isoniazid (b6 deficiency), bupropion, imipenem/cilastatin, tramadol, enflurane
(when i have a seizure I BITE my tongue)
these drugs cause tardive dyskinesia
antipsychotics, metoclopramide
these drugs cause diabetes insipidus
Li, demeclocycline
these drugs cause fanconi anemia
tenofovir, ifosfamide
these drugs cause hemorrhagic cystitis
cyclophosphamide, ifosfamide
these drugs cause SIADH
carbamazepine, cyclophosphamide, SSRIs
“Can’t Concentrate Serum Sodium”
these drugs cause pulmonary fribrosis
methotrexate,nitrofurantoin, carmustine, bleomycin, busulfan, amiodarone
(“My Nose Cannot Breathe Bad Air”)
these drugs cause disulfiram-like reaction
metronidazole, certain cephalosporins, griseofulvin, procarbazine, 1st generation sulfonylureas
these drugs cause nephrotoxicity/ototoxicity
aminoglycosides, vancomycin, loop diuretics, cisplatin (cisplatin toxicity may respond to amifostine)
P450 inducers
chronic alcohol, St. John’s wort, phenytoin, phenobarbital, nevirapine, rifampin, griseofulvin, carbamazepine
(“chronic alcoholics Steal Phen-Phen and Never Refuse Greasy Carbs”)
P450 substrates
anti-epileptics, theophylline, warfarin, OCPs
P450 inhibitors
acute alcohol, ritonavir, amiodarone, cimetidine/ciprofloxacin, ketoconazole, sulfonamides, INH, graprefruit juice, quinidine, macrolides (except azithromycin)
(“AAA RACKS IN GQ Magazine”)
these are sulfa drugs
sulfonamide antibx, sulfasalazine, probenecid, furosemide, acetazolamide, celcoxib, thiazides, sulfonylureas
-navir
protease inhibitor
-ovir
DNA polymerase inhibitor
-azine
typical antipsychotic
-etine
SSRI
-ipramine, -triptyline
TCA
-triptan
5HT 1b/1d agonist
-curium, -curonium
non-depolarizing paralytic
-stigmine
AChE inhibitor
-zosin
alpha 1 blocker
-afil
PDE-5 inhibitor
-dipine
dihydropyridine CCB
-xaban
direct factor Xa inhibitors
-dronate
bisphosphonate
-glitazone
PPAR-gamma activator
-prost
prostaglandin analog
-tidine
H2 blocker
-tropin
pituitary hormone
-ximab
chimeric mAb
-zumab
humanized mAb
effect of nore on CO, BP, HR and SVR
increase BP, SVR (main effect for both) unchanged CO decreased HR (reflex)
effect of epi on CO, BP, HR, and SVR
increase CO, BP, HR
Decreased SVR
effect of isoproteronol on CO, BP, HR, and SVR
significantly increases CO, HR (reflex) decreases BP (beta 2), SVR (beta 2)
these drugs cause acute cholestatic hepatitis and jaundice
erythromycin
P450 effect: chronic alcohol, st. john’s wort
stimulators
P450 effect: acute alcohol abuse, ritonavir
inhibitors
P450 effect: amiodarone, cimetidine
inhibitors
P450 effect: ciprofloxacin, ketoconazole
inhibitors
P450 effect: phenytoin, phenobarbital
stimulators
P450 effect: sulfonamides, INH
inhibitors
P450 effect: nevirapine, rifampin
stimulators
P450 effect: graprefuri juice, quinidine
inhibitors
P450 effect: macrolides
inhibitors (except azithromycin)
P450 effect: griseofulvin, carbamazepine
stimulators