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Pharm > Lecture 5 > Flashcards

Lecture 5 Flashcards

1
Q

What protein do acidic drugs bind to?

A

albumin

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2
Q

What protein do basic drugs bind to?

A

Alpha1-acid

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3
Q

Only what type of drug can act on targets and elicit a biologic response?

A

Unbound

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4
Q

What is involved in the 2nd phase of drug metabolism?

A

Conjugation with a 2nd endogenous substrate

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5
Q

How is valproic acid metabolized?

A

Hepatic via glucuronidation (conjugation)

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6
Q

What drug is the only P450 inhibitor in the antiepileptic class?

A

Valproic acid

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7
Q

Is the relationship b/w dose and total valproate concentration linear or non-linear?

A

Non-linear

Concentration doesn’t increase proportionally with the dose but increases to a lesser extent due to plasma binding

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8
Q

When you use carbamazepine with what other drug will you have a higher free fraction of carbamazepine?

A

Valproate sodium

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9
Q

What is the one active metabolite that eliminates carbamazepine?

A

carbamazepine 10,11 epoxide

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10
Q

What is carbamazepine primarily metabolized by?

A

CYP3A4

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11
Q

Carbamazepine has _____ induction; it induces it’s own metabolism.

A

auto

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12
Q

What happens to the half-life of carbamazepine after about 3-5 weeks?

A

Drops because it is inducing its own metabolism

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13
Q

What is warfarin’s onset of action?

A

24-72 hours

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14
Q

When is Warfarin’s peak effect?

A

5-7 days (INR increases in 36-72 hours)

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15
Q

What is Warfarin metabolized by?

A

CYP2C9

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16
Q

If you are heterozygous for reduced function of CYP2C9 what happens with warfarin metabolism?

A

Warfarin doesn’t metabolize well

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17
Q

Where is digoxin absorbed?

A

Small intestine (via passive non-saturable diffusion)

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18
Q

Digoxin distributes very nicely to where?

A

The heart (serum concentration of 70:1)

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19
Q

How long does the distribution phase of digoxin last?

A

6-8 hours

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20
Q

Digoxin has a very _____ therapeutic index.

A

Narrow (0.5-0.8 ng/mL)

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21
Q

When is digoxin toxic?

A

> 2ng/ mL

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22
Q

Patients with variation in ________ have a decreased rate of metabolism of succinylcholine resulting in prolonged paralysis after drug exposure (anesthesia).

A

BChE (butyrlcholinesterase)

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23
Q

A slow acetylator phenotype of N-acetyltransferase 2 (NAT2) is associated with drug ______.

A

toxicities

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24
Q

What drugs does NAT2 catlyze the acetylation of?

A

Isoniazid, Hydroalazine, Procainamide

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25
Q

What are some meds that are metabolized by CYP2D6?

A

Metoprolol
Haloperidol
Codeine
Fluoxetine

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26
Q

What are the three types of metabolizers for CYP2D6?

A

Poor (caucasians)
Extensive
Ultra-rapid (Ethiopians, Spaniards)

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27
Q

If a ultra-rapid CYP2D6 metabolizer gets codeine what will it be metabolized quickly into?

A

morphine –> Heroin

Normal codeine can result in OD

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28
Q

Codeine is relatively ineffective in ______ CYP2D6 metabolizers.

A

Poor

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29
Q

Thiopurine S-Methyltransferase (TPMT) catalyzes the S-Methylation of thiopurine drugs such as __________ and ___________

A

mercaptopurine

Azathioprine immunosuppressant agents

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30
Q

What does TPMT*3A result in?

A

Decrease in tissue level of TPMT

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31
Q

Patient’s homozygous for TPMT*3A are at a greatly increased risk for ______________ when treated with a standard dose of thiopurine drugs.

A

life threatening myelosuppression

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32
Q

What is a drug target for the asthma drug Zileuton?

A

5-lipoxygenase

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33
Q

What does ZIleuton do?

A

Decreases airway inflammation by inhibiting 5-lipoxygenase

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34
Q

5-lipoxygenase is encoded by what gene? What is the most common ALOX5 repeat variations?

A

ALOX5; 5 repeats is most common

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35
Q

Only people with at lest ???? copy(ies) of the five-repeat allele respond to zileuton therapy?

A

one copy

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36
Q

What is warfarin’s target?

A

Vitamin K epoxide reductase

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37
Q

What gene encodes Vitamin K epoxide reductase?

A

VKORC1 (vitamin K epoxide reductase complex 1)

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38
Q

What type of warfarin is metabolized predominately by CYP2C9?

A

S-Warfarin

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39
Q

What seems to result from interactions between the medication and a unique aspect of the physiology of the individual patient?

A

Idiosyncratic rxns

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40
Q

HLA-B*5701 is associated with ________ induced hypersensitivity.

A

Abacavir (reverse-transcriptase inhibitor)

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41
Q

these are cardiovascular afferents. Respond to changes in BP. Found in aortic arch and carotid sinus.

A

Cardiovascular afferents

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42
Q

Nociceptive nerusons follow _______ nerves.

A

Sympathetic

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43
Q

In the ANS, which is myelinated- preganglionic neuron or postganglion neuron?

A

Preganglionic neuron

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44
Q

This innervates the GI tract, pancreas and gallbaldder.

A

Enteric portion of the autonomic nervous system

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45
Q

The preganglionic neuron neuron to where doesn’t have a postgnaglionic neuron.

A

To adrenal medulla

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46
Q

What is released when the preganglionic neuron stimulates the adrenal medulla.

A

Epi

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47
Q

This type of chemical signaling is rapidly destroyed and doesn’t enter the blood.

A

Local mediators

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48
Q

This type of chemical signaling is by endocrine cells into the blood. It exerts effects on targets throughout the body.

A

Hormones

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49
Q

What are the 5 key steps of neurotransmission?

A 
Synthesis of neurotransmitter
Storage of neurotransmitter
Release of neurotransmitter
Recognition of neurotransmitter
Metabolism of neurotransmitter
50
Q

The parasympathetic system synthesizes and uses what NT?

A

Acetylcholine (ach)- is call cholinergic

51
Q

What receptors does Ach interact with?

A

Muscarinic

Nicotinic

52
Q

What NT does the sympathetic system use?

A

Norepinephrine (NE) is called adrenergic

53
Q

What receptors does norepienprhine interact with?

A

alpha andrenergic and beta adrenergic receptors

54
Q

Arterioles, veins, and sweat glands have a predominant what tone (ANS)?

A

Sympathetic

55
Q

Sweat glands have a sympathetic tone but are mediated by what?

A

Muscarinic mechanism (type of cholinergic receptor)

56
Q

Cholinergic Pharmacology is centered on what NT?

A

Ach

57
Q

WHat does cholinergic pharmacology involve?

A

NMJ
ANS
CNS

58
Q

What is the precursor of Ach?

A

choline

59
Q

What transports choline from the plasma into the nerve cell?

A

Na+ dependent carrier

60
Q

What inhibits choline transport?

A

Hemicholinium

61
Q

Choline + Acetyl CoA in the presence of what leads to the production of Ach?

A

Choline acetyltransferase (CAT)

62
Q

Ach is trasnported into synaptic vesicles via what?

A

Proton antiporter (protected from degradation)

63
Q

What causes the release of Ach?

A

Action potentials of Calcium influx –> release of vesicles through exocytosis

64
Q

What blocks the release of Ach?

A

Botulinum toxin

65
Q

What exogenous substance causes the release of Ach?

A

Spider venom

66
Q

What enzyme is present in cholinergic synapses and rapidly converts Ach.

A

Acetylcholinesterase (AChE)

67
Q

What does AchE convert Ach into?

A

choline and acetic acid

68
Q

What is an enzyme that is less specific for Ach and is found throughout the body.

A

BuChE (butylcholinesterase)

69
Q

M1 receptors are found where?

A

Neural: CNS, PNS, gastric parietal cells

70
Q

M2 receptors are found where?

A

Cardiac, bladder, lung

71
Q

M3 receptors are found where?

A

Glandular: exocrine glands, smooth muscles, bladder, and also eye

72
Q

What M receptors are coupled to G-proteins and responsible for Stimulation of phospholipase C

A

M1, M3, and M5

73
Q

What receptors are coupled to G-proteins responsible for adenyl cyclase inhibition and K+ channel activation?

A

M2 and M4

74
Q

What nicotinic receptors are at autonomic ganglia?

A

N2 or Nn

75
Q

What nicotinic receptors are at NMJ- somatic motor end plates?

A

N1 and Nm

76
Q

Where are binding sites for Ach?

A

Preganglionic synpases of both sympathetic and parasympathetic ganglia (Nm, M1, M2, M3)
parasympathetic postganglonic neuroeffector junctions
All somatic end-plates of skeletal muscle (nM)

77
Q

What muscarinic receptor decreases heart rate?

A

M2

78
Q

What muscarinic receptor does all the other function except decrease HR ?

A

M3

79
Q

Activation of muscarinic receptor of the eye leads to what?

A

Contraction of spinchter muscle of iris and ciliary muscle.

80
Q

What does activation of the muscarinic receptors of the GI lead to?

A

Increased tone, motility and secretion.

81
Q

What response does activation of muscarinic receptors of the secretory glands lead to?

A

Increased secretion

82
Q

What does activation of muscarinic receptors of the urinary bladder lead to?

A

Relaxation of the sphincter

83
Q

What are two direct-acting receptor agonists of cholinomimetic drugs?

A

Choline esters

Alkaloids

84
Q

What cholinergic agonists are hydrolyzed by AchE?

A

Ach

Methacholine

85
Q

What cholinergic agonists aren’t hydrolyzed by AchE?

A

Carbachol
Bethanechol
Muscarine
Pilocarpine

86
Q

What cholinergic agonists are specific only for muscarinic recpetors?

A

Bethanechol
Muscarine
Pilocarpine

87
Q

What cholinergic agonists have specificity for both muscarinic and nicotinic receptors?

A

Ach
Carbachol
Methacholine

88
Q

Is methacholine more specific for mAChR or nAChR?

A

mAChR

89
Q

Does carbachol have more receptor specificity for mAChR or nAChR?

A

nAChR

90
Q

Which choline ester has the largest pharmacological action on the CV system?

A

Metacholine

91
Q

The stimulation of ____ receptor on endothelial cells releases endothelium-derived relaxing factor _______ to produce dilation of all vascular bed?

A

Stimulation of M3 receptor

Relaxing factor- nitric oxide

92
Q

Coronary vasodilation may be elicited by direct electric stimulation of what nerve?

A

Vagus

93
Q

Cholinergic stimulation affect cardiac function directly by inhibiting effects of what?

A

Adrenergic activation

94
Q

cholinergic stimulation leads to a decrease in the force of what?

A

Cardiac contraction (negative inotropic effect)

95
Q

Cholinergic stimulation leads to a decrease in the rate of conduction in specialized tissues where?

A

SA and AV nodes (negative chronotropic effect)

96
Q

What receptors does bethanechol act at?

A

M1, M2, M3

97
Q

What sites does bethanechol work at?

A

smooth musculature of the bladder, and GI

Increases intestinal motility and tone and stimulates detrusor muscles of the bladder

98
Q

What are some therapeutic applications of bethanechol?

A

Stimulate the atonic bladder postpartum or postoperative urinary retention
Treat Postoperative abdominal distension and gastric atony and retention

99
Q

What are some ADR of bethanechol?

A

sweating, salvation, flushing, HPOTN, N/D, abdominal pain, bronchospasm

100
Q

What drug is used as an alteranative to pilocarpine to promote salivaiton in Sjogren syndrome?

A

Bethanechol

101
Q

How long is the DOA of carbachol (carbamylcholine)?

A

As long as 1 hour

102
Q

What receptors does carbachol activate?

A

M1, M2, M3, weak nicotinic agonist

103
Q

Since carbachol is a weak nicotinic agonist what will it don on the CV and GI systems?

A

May 1st stimulate then depress

104
Q

Carbachol may also cause the release of ______ from the ________ by its nicotinic actions.

A

Epinephrine from the adrenal medulla

105
Q

What is the therapeutic applications of carbachol?

A

Rarely used

Sometimes used as miotic for glaucoma

106
Q

What are the ADRs of carbachol ?

A

Little or no side effects when used in the eye.

107
Q

What receptors does Methacholine activate?

A

M1, M2, M3

108
Q

What is methacholine used for?

A

Diagnostic for bronchial hyperreactivity and asthmatic conditions

109
Q

_______ acts almost eclusively at muscarinic receptor sites

A

Muscarine

110
Q

Arecoline acts at what type of receptor?

A

Nicotine receptors

111
Q

_________ has a dominant muscarinic action, but causes anomalous CV responses, and sweat glands particularly sensitive to drug

A

Pilocarpine

112
Q

What receptors does pilocarpine act at?

A

M1, M2, M3

113
Q

This drug is an alkaloid and a tertiary amine. It is less potente than other cholinomemtic drugs and is hydrolyzed by AchE?

A

Pilocarpine

114
Q

What is the therapeutic use of pilocarpine?

A

Emergency lowering of intraocular pressure in both wide and narrow angle glaucoma.

115
Q

What are some ADRs of pilocarpine?

A

CNS effects

Profuse sweating and salivation

116
Q

What is the antidote of Ach and its agonists analogs?

A

Atropine

117
Q

What are the only ways Ach and its agonists should be administered?

A

Oral of subcutaneous routes

118
Q

Why is asthma contraindicated with Ach and its agonists?

A

Bronchoconstrictor action coudl precipitate asthmatic attack

119
Q

Why is hyperthyroidism contraindicated for Ach and its agonists?

A

May develop a-fib

120
Q

Why is coronary insufficiency contraindicated for Ach and its agonists?

A

hypotension induced by these agents can severely reduce coronary blood flow

121
Q

Why is peptic ulcer disease contraindicated for Ach and its agonists?

A

Gastric acid secretion producted by choline esters can aggravate symptoms

122
Q

What are some undesirable effects of Ach and its agonsits analogs?

A 
Flushing
Sweating
Abdominal cramps
Sensation of tightness in urinary bladder
Difficulty in visual accomodation
headache
salivation

Pharm (29 decks)

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