Pharmacology Flashcards
(87 cards)
1
Q
Km
A
inversely related to the affinity of the enzyme for its substrate
2
Q
Vmax
A
directly proportional to the enzyme concentration
3
Q
Line-weaver burk plot
A
X intercept = 1/-Km
Y intercept = 1/Vmax
slope = Km/Vmax
4
Q
Volume of distribution
A
Vd = amount of drug in body/ plasma concentration
- Vd low if drug is in the blood only, med if in the interstitial space, and high if in all tissues including fat
5
Q
half life
A
- drugs infused at a constant rate take 4-5 HL to reach steady state
- takes 3.3 HL to reach 90% steady state levels
6
Q
zero vs. first order elimination
A
- zero = constant amount cleared per unit time
- PEA - phenytoin, ethanol, aspirin
- first = constant fraction cleared per unit time
7
Q
weak acid drugs and urine pH
A
- phenobarb, methotrexate, aspirin
- trapped in basic environment, treat overdose with bicarb
8
Q
weak base drugs and urine pH
A
- amphetamines
- trapped in acidic environment, treat overdose with ammonium chloride
9
Q
therapeutic index
A
TD50/ED50
median toxic dose/median effective dose
10
Q
parasympathetic innervation of cardiac smooth muscle, gland cells and nerve terminals
A
- Ach at nicotinic receptor at ganglion
- Ach at muscarnic receptor at tissue
11
Q
sympathetic innervation of sweat glands
A
- Ach at nicotinic receptor at ganglion
- Ach at muscarinic receptor at tissue
12
Q
sympathetic innervation of cardiac smooth muscle, gland cells and nerve terminals
A
- Ach at nicotinic receptor at ganglion
- NE at alpha/beta receptor at tissue
13
Q
sympathetic innervation of renal vasculature and smooth muscle
A
- Ach at N receptor at ganglion
- Dopamine at D1 receptor at tissue
14
Q
sympathetic innervation of adrenal medulla
A
- Ach at N receptors stimulates it to release Epi and NE
15
Q
somatic innervation of skeletal muscle
A
- Ach directly at N receptors at tissue
16
Q
alpha1 receptor
A
- Gq receptor
- inc vascular smooth muscle contraction, inc pupillary dilator contraction, inc intestinal and bladder sphincter muscle contraction
17
Q
a2 receptor
A
- Gi receptor
- decreases sympathetic outflow, dec insulin release, dec lipolysis, inc platelet aggregation
18
Q
b1 receptor
A
- Gs receptor
- inc HR, contractilty, renin release, lipolysis
19
Q
b2 receptor
A
- Gs receptor
- vasodilation, bronchodilation, inc HR, contractility, lipolysis, insulin release
- decreased uterine tone, ciliary muscle releaxation, inc aqueous humor production
20
Q
M1 receptor
A
- Gq receptor
- CNS, enteric nervous system
21
Q
M2 receptor
A
- Gi receptor
- decreased HR and contractility of atria
22
Q
M3 receptor
A
- Gq receptor
- inc exocrine gland secretions, inc gut peristalsis, inc bladder contraction, bronchoconstriction, inc pupillary sphincter muscle contraction, ciliary muscle contraction
23
Q
D1 receptor
A
- Gs receptor
- relaxes renal vascular smooth muscle
24
Q
D2 receptor
A
- Gi receptor
- modulates transmitter release, esp in brain
25
H1 receptor
- Gq receptor
| - inc nasal and bronchial mucus production, inc vascular permeability, contraction of bronchioles, pruritis and pain
26
H2 receptor
- Gs receptor
| - inc gastric acid secretion
27
V1 receptor
- Gq receptor
| - inc vascular smooth muscle contraction
28
V2 receptor
- Gs receptor
- inc H20 permability and resorption in the collecting tubules of the kidney
- V2 is found in the 2 kidneys
29
which receptors are paired with which G proteins
```
HAVE 1 M and M --- Gq
- H2, a1, V1, M1 and M3
MAD 2s ----- Gi
- M2, a2, D2
all the rest work on Gs
```
30
bethanecol
- cholinomimetic drug used for post op ileus, neurogenic ileus and urinary retention
- activates Bowel and Bladder smooth muscle, resistant to AchE
- "bethany call me maybe if you want to move your bowel or bladder"
31
carbachol
- cholinomimetic agent used for glaucoma, pupillary constriction, and relief of intraocular pressure
- "CARBon copy of AcetylCHOLine"
32
pilocarpine
potent stimulator of sweat, tears and saliva
- used for open and closed angle glaucoma
- "you cry, drool and sweat on your PILOw"
33
neostigmine
- postop and neurogenic ileus and urinary retention, myasthenia gravis, reversal of NMJ blockade
- inc endogenous Ach
- Neo = No CNS penetration
34
pyridostigmine
-myasthenia gravis (long acting), does not penetrate the CNS
35
physostigmine
- anticholinergic tox (crosses BBB)
36
donepezil, rivastigmine, galantamine
Alzheimers
| - inc endogenous Ach
37
edrophonium
- diagnosis of MG
| - increases endogenous Ach
38
cholinesterase inhibitor poisoning (organophosphates)
DUMBBELSS
- diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of skeletal muscle and CNS, Lacrimation, Sweating, Salivation
39
atropine, homatripine, tropicamide
muscarinic antagonists that act on the eye
| - produce mydriasis and cycloplegia
40
benztropine
- muscarinic antagonist that acts on the CNS
| - parkinson's disease/pyramidal SE of psych meds
41
scopolamine
- muscarinic antagonist that acts on the CNS
| - motion sickness
42
oxybutynin
- muscarinic antagonist that acts on GU
| - reduces urgency
43
glycopyrrolate
- muscarinic antagonist that acts on GI and resp
- parenteral: preop use to reduce airway secretions
- oral: drooling, peptic ulcer
44
atropine
- muscarinic antagonist. used to treat bradycardia and for ophthalmic applications
- inc pupil dilation, dec airway secretions, dec acid secretion, dec GI motility, dec urgency in cystitis (blocks DUMBBELSS)
- tox: hot as a hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter
45
epinephrine
- beta > alpha
- anaphylaxis, open angle glaucoma, asthma, hypotension, alpha effects predominate at high doses
- inc HR, SBP, dec DBP at low doses, inc DBP at high doses
- if alpha blockers given before, net depressor effect
46
norepi
- alpha1 > alpha2 > beta1
| - hypotension (but dec renal perfusion)
47
isoproterenol
- B1 = B2
| - electrophysiologic eval of tachyarrhythmias, can worsen ischemia
48
dopamine
- D1 = D2 > beta > alpha
| - unstable bradycardia, HF, shock, inotropic and chronotropic alpha effects predominate at high doses
49
dobutamine
- B1 > B2, alpha
| - heart failure (inotropic > chronotropic), cardiac stress testing
50
phenylephrine
alpha1 > alpha2
- hypotension, ocular procedures, rhinitis
- if alpha blockers given before, no pressor effect
51
albuterol, salmeterol, terbutaline
- B2 > B1
| - asthma, COPD control, and reduce uterine contractions, respectively
52
amphetamine
- indirect general sympathomimetic, reuptake inhibitor, also releases stored catecholamines
- applications in narcolepsy, obesity, ADD
53
ephedrine
- indirect general sympathomimetic, releases stored catecholamines
- used for nasal decongestion, urinary incontinence, and hypotension
54
cocaine
- indirect general sympathomimetic, reuptake inhibitor
| - vasoconstriction and local anesthesia
55
clonidine
- a2 agonist for hypertensive urgency, ADHD, severe pain
| - tox: CNS depression, bradycardia, hypotension, respiratory depression and small pupils
56
methyldopa
- HTN in preggos
| - tox: direct coombs +, SLE-like syndrome
57
phenoxybenzamine
irreverible nonselective alpha blocker
- used to treat pheo
- tox: orthostatic hypotension, reflex tachy
58
phentolamine
reversible nonselective alpha blocker
| - give to pts on MAOis who eat foods with tyramine
59
prazosin, terazosin, doxazosin, tamsulosin
selective alpha 1 blockers used for BPH
- prazosin for PTSD
- tox: 1st dose orthostatic hypotension, dizziness, headache
60
mirtazepine
selective alpha 2 blocker for depression
| - increases sedation, serum cholesterol and appetite
61
b1 selective beta blockers
- acebutolol, atenolol, betaxolol, esmolol, metoprolol
| - A--> M (1st half of alphabet)
62
non-selective beta blockers
nadolol, pindolol, propranolol, timolol
| - N to Z, second half of alphabet
63
non-selective alpha and beta antagonists
cavedilol and labetalol
| dont end in the typical olol
64
antimuscarinic OD treatment
physostigmine salicylate, control hyperthermia
65
AchE inhibitors, organophosphate OD treatment
atropine followed by pralidoxime
66
copper, arsenic, gold OD treatment
penicillamine
67
digitalis OD treamtnet
anti-dig Fav fragments
68
cyanide OD treatment
nitrite + thiosulfate, hydroxocobalamin
69
iron OD treatment
deferoxamine, deferasirox
70
lead OD treatment
EDTA, dimercaprol, succimer, penicillamine
71
methanol, ethylene glycol poisoning
fomepizole > ethanol, dialysis
72
tPA, streptokinase, urokinase OD treatment
aminocaproic acid
73
drugs that cause flushing
VANC
| - vancomycin, adenosine, niacin, Ca channel blockers
74
drugs that cause hyperglycemia
Taking Pills Necessitates Having Blood Checked
| - tacrolimus, protease inhibitors, niacin, HCTZ, B blockers, corticosteroids
75
drugs that cause hypothyroidism
lithium, amiodarone, sulfonamides
76
drugs that cause hepatic necrosis
Liver "HAVAc"
| - halothane, Amanita phalloides (death cap mushroom), Valproic acid, Acetaminophen
77
drugs that cause agranulocytosis
Dapsone, Clozapine, Carbamezapine, Colchicine, Methimazole, Propylthiouracil
- Drugs CCCrush Myeloblasts and Promyelocytes
78
drugs that cause hemolysis in G6PD
hemolysis IS D PAIN
| - INH, sulfonamides, dapsone, primaquine, aspirin, ibuprofen, nitrofurantoin
79
drugs that cause photosensitivity
SAT For Photo
| - sulfonamides, amiodarone, tetracyclines, 5FU
80
SLE-like syndrome
- having lupus is "SHIPP-E"
- sulfa drugs, hydralazine, INH, procainamide, phenytoin, entanercept"
- also methyldopa
81
drugs that cause seizures
with seizures, I BITE My arm
| - INH, buproprion, imipenem/cilastatin, tramadol, enflurane, metoclopramide
82
P450 inducers
Chronic Alcoholic Mona Steals Phen-Phen and Never Refuses Greasy Carbs
- chronic alcohol use
- modafinil
- St. John's wart
- phenytoin
- phenobarb
- Nevirapine
- Rifampin
- Griseofulvin
- Carbamezapine
83
P450 inhibitors
```
A cute Gentleman "Cipps" Iced Grapefruit juice Quickly and Kept Munching on Soft Cinammon Rolls
acute alcohol abuse
gembifrozil
cipro
isoniazid
grapefruit juiice
quinidine
amiodarone
ketoconazole
macrolides
sulfonamides
cimetidine
ritonavir
```
84
P450 substrates
anti-epileptics, antidepressants, antipsychotics, anesthetics, theophylline, warfarin, statins, OCPs
-- Always, Always, Always, Always Think When Starting Others
85
sulfa drugs
Popular FACTSSS
| - probenecid, furosemide, acetazolamide, celecoxib, thiazides, sulfonamide abx, sulfasalazine, sulfonureas
86
Clearance calc
CL = rate of elimination/plasma drug conc
| = Vd x Ke
87
dosage calculations
loading dose = Cp x Vd / F
maintenance dose = Cp x CL x t / F
```
Cp = target plasma concentration
t = dosage interval
F = bioavailability
```
