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Flashcards in General/Autonomics Pharm Deck (85):
1

Difference in competitive vs noncompetitve inhibitors?

competitive = decrease potency, noncompetitive = decrease efficacy. Pharmacology General

1

What is Km?

Inverse relation of affinity of enzyme for its substrate. Pharmacology General

2

What is Vmax?

Direct proportion to enzyme concentration Pharmacology General

3

What is bioavailability?

Fraction of administered drug that reaches systemic circulation unchanged. Pharmacology General

4

Time to steady state depends on?

depends on half-life. Does not depend on frequency or size of dose. Pharmacology General

5

What is rate of elimination in zero order kinetics?

constant amount eliminated per time. Pharmacology General

6

Give three drugs that are zero order eliminated.

PEA - phenytoin, Ethanol, Aspirin. Pharmacology General

7

What is the rate of elimination for first order kinetics?

A constant FRACTION is eliminted, variable by concentration! Pharmacology General

8

How does ionization relate to urine pH?

Ionzied species are trapped in urine and not resorbed. Neutral can be resorbed. Pharmacology general

9

How do you treat overdose of weak acid? Give drug examples.

Treat with Bicarb to make neutral. Exp: phenobarbital, methotrexate, aspirin. Pharmacology general

10

How do you treat overdose of weak base? Give drug examples.

Treat with ammonium chloride. exp: amphetamines. Pharmacology general

11

What is phase I drug metabolism? What pt. population loses this?

Reduction, Oxidation, hydrolysis with CYP450. Often gives neutral products. Geriatrics lose this phase. Pharmacology general

12

What is phase II metaboloism? What population depend on this?

Conjugation (Glucuronidation, Acetylation, and Sulfation.) Gives charged products. Geriatrics depend on this, old people have GAS. Pharmacology general

13

What is efficacy?

maximal effect a drug can produce. Pharmacology general

14

What is potency?

amount of drug needed for the same effect. Pharmacology general

15

What happends to efficacy when a partial agonist and full agonist are mixed?

DECREASED efficacy. fight for same binding site, full agonist cant exert full effect. Pharmacology general

16

What is therapetuic index?

LD50/ED50. Median lethal dose divded by median effective dose. Safer drugs have a higher TI. pharmacology general

17

What is a therapeutic window?

Minimum effective dose to minimum toxic dose. Think of it as range of use. pharmacology general

18

What are the two types of Nicotonic receptors? What kind of messenger do they use?

1. Nicotinic - Ligang gated Na/K channels. Two nicotinic types: Nm(NMJ) and Nn(autonomic ganglia. 2. Muscarinic - G-proteins. 5 types, M1-M5. pharmacology general

19

Alpha-1 sympathetic receptor (G-protein class, major function)

q, increase: vasc. smooth muscle contraction, pupillary dilator muscle contraction, intestinal and bladder sphincter contaction. pharmacology autonomics

20

Alpha-2 sympathetic receptor(G-protein class, major function)

i, decrease: sympathetic outflow, insulin release, lipolysis. increase: platlet aggregation. pharmacology autonomics

21

Beta-1 sympathetic receptor(G-protein class, major function)

s, increase: heart rate, contractilty, renin release, lipolysis pharmacology autonomics

22

Beta-2 sympathetic receptor(G-protein class, major function)

s, vasodilation, brochodilation, increase: heart rate, contractility, lipolysis, insulin release, aqueous humor production. decrease: uterine tone, ciliary muscle tone. pharmacology autonomics

23

M-1 Parasymp receptor(G-protein class, major function)

q, CNS, enteric nervouse system. pharmacology autonomics

24

M-2 Parasymp(G-protein class, major function)

i, decease: heart rate, contractility of atria pharmacology autonomics

25

M-3 parasymp(G-protein class, major function)

increase: exocrine gland secretion (tears, gastric, etc), gut peristalsis, bladder contraction, bronchoconstriction, pupillary spinchter contraction, cilliary muscle contraction. pharmacology autonomics

26

What receptor is responsible for miosis and accomadation?

Parasympathetic M-3. pharmacology autonomics

27

What receptor is responsbile for mydriasis?

Sympathetic Alpha-1. pharmacology autonomics

28

Dopamine D-1 receptor(G-protein class, major function)

s, relaxes renal vascular smooth muscle pharmacology autonomics

29

Dopamine D-2 receptor(G-protein class, major function)

i, modulates transmitter release especially in brain. pharmacology autonomics

30

Histamine H-1 receptor(G-protein class, major function)

q, increase: mucus production, contraction of bronchioles, pruritus, pain. pharmacology autonomics

31

histamine H-2 receptor(G-protein class, major function)

a, increase gastric acid secretion pharmacology autonomics

32

vasopression V-1 receptor(G-protein class, major function)

q, increase: vascular smooth muscle contraction pharmacology autonomics

33

vasopression V-2 receptor(G-protein class, major function)

s, increase water permeability and reabsorption in kidneys. (V2 found in 2 kidneys). pharmacology autonomics

34

Which receptors work via Gq -> Phospholipase C ->Pip2->DAG + IP3?

H1,Alpha1,V1,M1,M3. (remember HAVe 1 M&M) pharmacology autonomics

35

DAG causes activation of what?

Protein Kinase C. pharmacology autonomics

36

IP3 causes increase in what?

Calcium -> smouth muscle contraction pharmacology autonomics

37

Which receptors work via Gi->Adenyly cyclase ->cAMP ->Protein Kinase A?

M2, Alpha2, D2. (remember MAD 2's.) pharmacology autonomics

38

Which receptors work via Gs->adenylyate cyclase ->cAMP->Protein Kinase A?

Beta1, Beta2, D1, H2,V2. pharmacology autonomics

39

What does protein kinase A do?

increase calcium release in heart and blocks myosin light chain kinase. pharmacology autonomics

40

What are the two classes of cholinomimetics?

1. direct agonsts 2. indirect agonists (anticholinesterases). pharmacology autonomics

41

Bethanechol(mechanism,use,toxicity)

Direct cholinomimetic. Postop or neurogenic ileus, urinary retention. COPD+asthma exacerbation, peptic ulcers. pharmacology autonomics

42

Carbachol(mechanism,use,toxicity)

Direct Cholinomimetic. Identical to Ach. Glaucoma, pupillary contraction, relief of IOP. COPD+asthma exacerbation, peptic ulcers. pharmacology autonomics

43

Pilocarpine(mechanism,use,toxicity)

Direct Cholinomimetic. Stimulates tears, salvia, sweat. Open and closed-angle glaucoma.COPD+asthma exacerbation, peptic ulcers. pharmacology autonomics

44

methacholine(mechanism,use,toxicity)

Direct Cholinomimetic. challenge test of asthma diagnosis. COPD+asthma exacerbation, peptic ulcers. pharmacology autonomics

45

Neostigmine(mechanism,use,toxicity)

Indirect cholinomimetic agonist. NO cns penetration. Postop and neurogenic ileus, myasthenia gravis, reversal of NMJ block. COPD+asthma exacerbation, peptic ulcers. pharmacology autonomics

46

pyridostigmine(mechanism,use,toxicity)

indirect cholinomimetic agonist. Long acting myasthenia gravis treatment. COPD+asthma exacerbation, peptic ulcers. pharmacology autonomics

47

edrophonium(mechanism,use,toxicity)

indirect cholinomimetic agonist. Short acting, for myasthenia gravis diagnosis. COPD+asthma exacerbation, peptic ulcers. pharmacology autonomics

48

Physostigmine(mechanism,use,toxicity)

indirect cholinomimetic agonist. for anti-cholinergic overdose, crosses BBB. COPD+asthma exacerbation, peptic ulcers. pharmacology autonomics

49

Donepezil(mechanism,use,toxicity)

indirect cholinomimetic agonist. Alzheimers disease. COPD+asthma exacerbation, peptic ulcers. pharmacology autonomics

50

signs of cholinesterase inhibitor poisoning. treatment.

DUMBBELSS (diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of skeletal muscle +CNS, lacrimation, sweating, salvia.) tx: atropine + pralidoxime. pharmacology autonomics

51

Parathion(mechanism, treatment)

Irreversible cholinesterase inhibitor, ACH overdose. Tx: atropine + pralidoxime. pharmacology autonomics

52

Atropine, homatropine, tropicamide (mechanism, use, toxicity).

Muscarinic antagonist. produces mydriasis and cycloplegia. (Atropine also used for bradycardia). Causes hot as a hare, dry as bone, red as beet, blind as bat, mad as a hatter. pharmacology autonomics

53

Benztropine(mechanism,use,toxicity)

Muscarinic antagoist. Parkinsons disease (park my benz). Causes hot as a hare, dry as bone, red as a beet, blind as a bat, mad as a hatter. pharmacology autonomics

54

Scopolamine(mechanism,use,toxicity)

Muscarinic antagonist. Motion sickness. causes hot as a hare, dry as a cone, red as a beet, blind as a bat, mad as a hatter. pharmacology autonomics

55

Ipratropium,tiotropium (mechanism, use, toxicity)

Muscarinic antagonist. COPD, Asthma. Causes hot as a hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter. pharmacology autonomics

56

Oxybutynin(mechanism,use,toxicity)

Muscarinic anatagonist. reduces urgency in mild cystitis and reduce bladder spasms. causes hot as a hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter.

57

Glycopyrrolate(mechanism,use,toxicity)

Muscarinic anatagonist. IP: given in preop to reduce airway secretions. oral:reduce drooling, peptic ulcer. Can cause hot as a hare, dry as a bone red as a beet, blind as a bat, mad as a hatter. pharmacology autonomics

58

Jimson Weed(mechanism, toxicity)

muscarinic antagonist, causes gardner's pupil (mydriasis). pharmacology autonomics

59

Epinephrine(Mechanism, receptors bound, use, toxicity)

Direct Sympathomemetic. A1,A2,B1,B2. Anaphylaxis, open angle glaucoma, asthma, hypotension. pharmacology autonomics

60

Norepinephine(Mechanism, receptors bound, use, toxicity)

direct sympathomemetic. A1,A2, some B1. used in hypotension but it decrease renal perfusion. pharmacology autonomics

61

Isoproterenol(Mechanism, receptors bound, use, toxicity)

Direct sympathomemetic. B1, B2. Used in Torsade de pointe and bradyarryhmia. Can cause tachycardia and worsen cardiac ischemia. pharmacology autonomics

62

dopamine(Mechanism, receptors bound, use, toxicity)

Direct sympathomimetics. Receptors depend on dose. low = D1, med = D1,B2,B1, high = A1,A2,B1,B2,D1. Used in shock and heart failure (ionotropic and chronotropic). pharmacology autonomics

63

dobutamine(Mechanism, receptors bound, use, toxicity)

Direct sympathomimetic. Mostly B1, little a1,a2,b2. Used in heart failure and cardiac stresstest (ionotrpic and chronotropic) pharmacology autonomics

64

Phenylephrine(Mechanism, receptors bound, use, toxicity)

Direct sympathomimetic. A1, A2. Used in hypotension, to cause mydriasis, and rhinitis (decongestant). pharmacology autonomics

65

Albuterol, salmetrol, terbutaline (Mechanism, receptors bound, use, toxicity)

Direct sympathomimetic. Mostly B2, some b1. Sal = long term ashtma or copd. Albuterol for short term asthma. Terbutaline for to reduce premture uterine contractions. pharmacology autonomics

66

Ritodrine(Mechanism, receptors bound, use, toxicity)

Direct sympathomimetic. B2 only. Used to reduce premature uterine contractions. pharmacology autonomics

67

Amphetamine (mechanism, use)

indirect sympathomimetic. Releases stored catecholamines. Used for narcolepsy, obesity, ADD. pharmacology autonomics

68

Epinephrine(Mechanism, use, toxicity)

indirect sympathomimetic. Releases stored catecholamines. Used for nasal decongestion, urinary incontience, hypotension. pharmacology autonomics

69

Cocaine (mechanims, use).

direct sympathomimetic. Reuptake inhibitor. Causes vasoconstriction and local anesthesia. pharmacology autonomics

70

Why must B-Blockers be avoided in suspected cocaine intoxication?

mixing them can lead to unopposed A1 activation and extreme hypertenion. pharmacology autonomics

71

How does norepinephrine cause reflex bradycardia?

stimulates A1>B2. Causes increased vasoconstrciton -> increased BP. This causes reflex bradycardia and slowing of HR. pharmacology autonomics

72

How does isoproterenol cause reflex tachycardia?

Stimulates B2>A1. This cause vasodilation and dropping of BP. B1 is stimulated and causes tachycardia. pharmacology autonomics

73

Clonidine, alpha-methyldopa(Mechanism, receptors bound, use)

Centrally acting alpha-2 agonists, this causes LESS peripheral sympathetic release.Used in hypertension, especially renal disease due to no increase in renal blood flow! pharmacology autonomics

74

Phenoxybenzamine(Mechanism, receptors bound, use, toxicity)

IRREVERSIBLE nonslective alpha blocker. Used in pheochromosytoma BEFORE surgery! toxic: orhtostatic hypotension, reflec tachycardia. pharmacology autonomics

75

phentolamine(Mechanism, receptors bound, use, toxicity)

REVERSBILE nonselective alpha blocker. give to patients on MAOI who each tyramine contraining foods. pharmacology autonomics

76

Prazosin, Terazosin, Doxazosin,Tamsulosin(Mechanism, receptors bound, use, toxicity)

Alpha-1 blocker. Used in hypertension, urinary rentention in BPH. tox:orthostatic hypotension, dizziness, headache. pharmacology autonomics

77

Mirtazapine (mechanism, use, toxicity)

Alpha-2 blocker. Used in depression. tox: sedation, hypercholesterolemia, increased apetite. pharmacology autonomics

78

Describe what occurs when you alpha-blockade epi vs. phenylephrine.

Before blockade: Both epi and phen RAISES BP. After alpha blockade: only epi raises, no change in phenyl. Why: Epi has B binding, phenyl does NOT. pharmacology autonomics

79

Give 6 applications of Beta-blockers in general.

Angina - decreases HR and contractility, decreasing oxygen use. MI - decrease mortality. SVT - decrease AV duction. Hypertension - decrease CO and renin secretion. CHF - slows progression. Glaucoma - decrease secretion of aqueous humor. pharmacology autonomics

80

give general toxicites of b-blockers

impotence, asthma exacerbation, bradycardia, seizures, sedation, hides hypoglycemia. pharmacology autonomics

81

What are the B1 selective b-blockers? When are they useful?

A BEAM. acebutolol, betaxolol, Esmolol, Atenolol, Metoprolol. Useful in comorbid pum. disease. pharmacology autonomics

82

What are the nonselective ( b1 = b2) b-blockers?

Please Try Not Being Picky. Propranolol, Timolol, Nadolol, Pindolol. B = B-blocker. pharmacology autonomics

83

what are the nonselective a and b-antagonists?

Carvedilol, labetalol. pharmacology autonomics

84

What are the partial B-agonists?

Pindolol, Acebutolol. pharmacology autonomics