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Pharm > Fundamentals > Flashcards

Fundamentals Flashcards

1
Q

Nm receptors

A

Neuromuscular junction; transient depolarization with increased Na/K

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2
Q

Nn receptors

A 
Autonomic ganglia (transient depolarization)
Adrenal medulla (increase internal Ca)
CNS (increase internal Ca)
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3
Q

Difference between nicotinic and muscarinic receptors

A 
Nicotinic = ligand-gated ion channels
Muscarinic = GTP-binding protein-linked receptors with secondary messengers
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4
Q

M1

A

Autonomic ganglia, CNS (Gq, PI turnover, increased Ca, increased cAMP)

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5
Q

M2

A 
Cardiac mm (hyperpolarization, increase K conductance, Gi, decrease cAMP)
CNS, presynaptic terminals
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6
Q

M3

A

Smooth mm, secretory glands, CNS (Gq, PI turnover, increased Ca, increased cAMP)

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7
Q

M4

A

CNS (Gi, decrease cAMP)

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8
Q

M5

A

CNS (Gq, PI turnover, increased Ca, increased cAMP)

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9
Q

T/F: clinically useful receptor subtype-specific agonists (ie Nm or M2) exist

A

FALSE

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10
Q

Curare

A

blocks Nm receptors

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11
Q

Heaxamethonium

A

blocks Nn (ganglionic) receptors

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12
Q

Atropine

A

blocks ALL muscarinic receptors

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13
Q

Rate of elimination

A

-keC [=] (mg/mL)/sec

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14
Q

Time course for drug concentration

A

= C0exp(-ket)

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15
Q

Half-life (t1/2 )

A

= 0.693/ke = 0.693Vd/CL

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16
Q

Volume of distribution (Vd )

A

= dose/Co = dose/(keAUC);[=] L/kg

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17
Q

Elimination rate

A

= CL x C [=] (mg/min/kg)

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18
Q

Dosage rate/infusion rate

A

= CL x Css

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19
Q

Multiple dose regimen (deltaCp)

A

= dose/Vd

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20
Q

Clearance

A

= ke x Vd = 0.693Vd/T1/2 [=] L/hr/kg

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21
Q

Infusion rate

A

= CL x Css = (0.693 x Vd)/T1/2 x Css [=] mg/kg/hr

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22
Q

Loading dose

A

= (Vd x Css)/bioavail.

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23
Q

Majority of drugs are metabolized by what phase I cytochromes?

A

CYP3A4 and CYP2D6

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24
Q

What do inducered increase?

A

SER

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25
Q

Important inducers of CYP2C9

A

barbituates (phenobarbital, phenytoin, primidone, rifampin)

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26
Q

Important inducers of CYP3A4

A

Barbituates, carbamazepine, cortixosteroids, efarirenz, phenytoin, rifampin, pioglitazone, St. Johns wort

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27
Q

3 important drugs that have zero-order kinetics

A

EtOH, aspirin and phenytoin

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28
Q

Important inhibitors of CYP2C9

A

Amiodarnon, chloramphenicol, cimetidine, isoniazid, metronidazole, SSRIs, zafirlukast

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29
Q

Important inhibitors of CYP3A4

A

Amiodarone, azole antifungals, cimetidine, clarithromycin, cyclosporin, erythromycin, flouroquinolnes, grapefruit juice, HIV protease inhibitors, metronidazole, quinine, SSRIs, tacrolimus

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30
Q

Rate limiting step of Ach production

A

transport of choline into the cell

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31
Q

Rate limiting step of dopamine production

A

tyrosine hydroxylation by tyrosine hydroxylase to DOPA

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32
Q

Sym and Para Function: Heart

A

b1 (increases HR, contractility, AV node conduction)

M2 (decreases HR, contractility, AV node conduction)

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33
Q

Sym and Para Function: Vascular smooth mm

A

a1 (contricts blood vessels in skin, splanchnic)
b2 (dilates blood vessels in skeletal mm)

NO Para function

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34
Q

Sym and Para Function: GI tract

A

a2/b2 (decrease motility)
a1 (constricts sphincters)

M3 (increase motility, relaxes sphincters)

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35
Q

Sym and Para Function: Bronchioles

A

b2 (dialates bronchiolar sm. mm)

M3 (constricts bronchiolar sm. mm)

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36
Q

Sym and Para Function: male sex organs

A

a (ejaculation)

M (errection)

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37
Q

Sym and Para Function: Bladder

A

b2 (relaxes bladder wall)
a1 (constricts sphincter)

M3 (contracts bladder wall and relaxes sphincter)

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38
Q

Sym and Para Function: Sweat glands

A

M (sympathetic cholinergic!!!) (increases sweating)

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39
Q

Sym and Para Function:Eye

A

a1 (dilates pupil - mydriasis)
b (relaxes/dilates ciliary mm for flattened lense, far vision)

M (constricts pupil - miosis, contracts ciliary mm for round lense, near vision)

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40
Q

Sym and Para Function:Kidney

A

b1 (increase renin secretion)

No PARA Component

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41
Q

Sym and Para Function: Fat cells

A

b1 (increase lipolysis)

No Para component

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42
Q

Where is there predominate sympathetic tone?

A

Arteries, veins, sweat glands

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43
Q

What other classes of drugs have anti-muscarinic activity?

A

Anti-histamines, anti-depressants (tricyclics), Phenothiazine antipsychotics, older neuromusclar blockers

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44
Q

Phentolamine

A

aAntagonist, Non-selective, a1 & a2 Reversible

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45
Q

Phenoxybenzamine

A

aAntagonist, Non-selective, a1 & a2 Reversible

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46
Q

Prazosin - prototype

A

aAntagonist, Selective a1

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47
Q

Terazosin

A

aAntagonist, Selective a1

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48
Q

Doxazosin - #1

A

aAntagonist, Selective a1

49
Q

Tamsulosin - new

A

aAntagonist, Selective a1

50
Q

Reserpine

A

Adrenergic Neuronal Blockers

51
Q

Guanethidine / Guanadrel

A

Adrenergic Neuronal Blockers

52
Q

Metyrosine

A

Adrenergic Neuronal Blockers

53
Q

Succinylcholine

A

Depolarizing competitive AChR agonist Rapid onset (1-2min), Short duration (5-15min)

54
Q

Tubocurarine

A

Non-depolarizing competitive AChR antagonist Slow onset, Long duration

55
Q

Metocurine

A

Non-depolarizing competitive AChR antagonist Slow onset, Long duration

56
Q

Pancuronium

A

Non-depolarizing competitive AChR antagonist Slow onset, Long duration (1-2 hr)

57
Q

Pipecuronium

A

Non-depolarizing competitive AChR antagonist Slow onset, Long duration

58
Q

Doxacurium

A

Non-depolarizing competitive AChR antagonist Slow onset, Long duration

59
Q

Vecuronium

A

Non-depolarizing competitive AChR antagonist Slow onset, Intermediate duration

60
Q

Atracurium

A

Non-depolarizing competitive AChR antagonist Slow onset, Intermediate duration

61
Q

Cisatracurium

A

Non-depolarizing competitive AChR antagonist Slow onset, Intermediate duration

62
Q

Rocuronium

A

Non-depolarizing competitive AChR antagonist Rapid onset, Intermediate duration (20-45min)

63
Q

Mivacurium

A

Non-depolarizing competitive AChR antagonist Rapid onset, Short duration

64
Q

Atropine

A

Anti-muscarinic, competitive mAChR antagonist, teritary amine - crosses BBB

65
Q

Tropicamide

A

Anti-muscarinic, competitive mAChR antagonist, teritary amine - crosses BBB

66
Q

Scopolamine

A

Anti-muscarinic, competitive mAChR antagonist, teritary amine - crosses BBB

67
Q

Propantheline

A

Anti-muscarinic, competitive mAChR antagonist, quatenary amine

68
Q

Ipratropium

A

Anti-muscarinic, competitive mAChR antagonist, quatenary amine

69
Q

Oxybutynin / Tolterodine

A

Anti-muscarinic, competitive mAChR antagonist

70
Q

Nicotine

A

Ganglionic blocker, depolarizing competitive nAChR agonist

71
Q

Mecamylamine

A

Ganglionic blocker, non-depolarizing competitive autonomic ganglia/nAChR agonist, teritary amine - crosses BBB

72
Q

Hexamethonium (C6)

A

Ganglionic blocker, non-depolarizing competitive autonomic ganglia/nAChR agonist, research only

73
Q

Tetraethylammonium

A

Ganglionic blocker, non-depolarizing competitive autonomic ganglia/nAChR agonist, research only

74
Q

Methacholine

A

Direct mAChR agonist, somewhat AChE-resistant

75
Q

Carbachol

A

Direct nAChR agonist, AChE-resistant

76
Q

Bethanechol

A

Direct mAChR agonist, AChE-resistant

77
Q

Pilocarpine

A

Direct partial mAChR agonist

78
Q

Edrophonium

A

Indirect anti-AChE, reversible competitive AChE antagonist

79
Q

Donepezil

A

Indirect anti-AChE, reversible competitive AChE antagonist, tertiary amine - crosses BBB

80
Q

Rivastigmine

A

Indirect anti-AChE, reversible competitive AChE antagonist - same as Donepezil, but 2x/day

81
Q

Galantamine

A

Indirect anti-AChE, reversible competitive AChE antagonist, most recent

82
Q

Physostigimine

A

Indirect anti-AChE, reversible competitive AChE substrate (slowly hydrolized) tertiary amine - crosses BBB

83
Q

Neostigmine

A

Indirect anti-AChE, reversible competitive AChE substrate (slowly hydrolized) quat. Amine

84
Q

Pyridostigmine

A

Indirect anti-AChE, reversible competitive AChE substrate (slowly hydrolized) quat. Amine

85
Q

Demecarium

A

Indirect anti-AChE, reversible competitive AChE substrate (slowly hydrolized)

86
Q

Echothiophate

A

Indirect anti-AChE, irreversible Organophosphate

87
Q

Parathion/Malathion

A

Indirect anti-AChE, irreversible Organophosphate

88
Q

Sarin/Soman

A

Indirect anti-AChE, irreversible Organophosphate

89
Q

Acebutolol

A

Aderenergic antagonist b1

90
Q

Atenolol

A

Aderenergic antagonist b1

91
Q

Esmolol

A

Aderenergic antagonist b1

92
Q

Metoprolol

A

Aderenergic antagonist b1

93
Q

Naldolol

A

Aderenergic antagonist b1 & b2

94
Q

Pindolol

A

Aderenergic antagonist b1 & b2

95
Q

Propranolol

A

Aderenergic antagonist b1 & b2

96
Q

Timolol

A

Aderenergic antagonist b1 & b2

97
Q

Sotalol

A

Aderenergic antagonist b1 & b2

98
Q

Labetalol

A

Aderenergic antagonist b1 & b2 & a1

99
Q

Therapeutic index

A

= (TD50/ED50)

100
Q

Margin of safety

A

= LD1/ED99

101
Q

Maintenance dose

A

= (CL x Css x dosing interval) / bioavil

102
Q

If there is no active secretion/reabsportion, then renal clearance is equal to what?

A

GFR

103
Q

Loading dose and maintenance does are effected by impaired renal or hepatic function how?

A

LD = (Vd x Css)/bioavail = STAYS THE SAME

MD = (CL x Css x dosing interval)/bioavail = DECREASES because is dept on CL

104
Q

What does high Vd mean

A

lots of drug in the tissue

105
Q

Types of transmembrane ion channels:

A

1) ligand gated channels (NMJ)
2) voltage gated channels (propagating of neural depol)
3) second messenger regulated gated channels (Muscarinic receptors activating IP3 which opens Ca+ gated channels)

106
Q

Types of GPCR

A

1) Gs - activated AC increases cAMP
2) Gi - inactivates AC decreases cAMP
3) Gq - activates Phos. lipase C which hydrolizes PIP2 to IP3 (increase intracellular Ca++) + DAG (activates Protein Kinase C)

107
Q

Types of Transmembrane receptors with enzymatic cytosolic domains?

A
  1. Tyrosine kinase receptors - kinase activity on their cytosolic domains which dimerize and phosphorylate each other as well as other proteins in the cell (Insulin and BCR-Abl protein)
  2. Receptor tyrosine phosphatases - phosphatase activity in the
    cytoplasmic domain and inhibits activation tyrosine kinase receptor. One receptor in this class dephosphorylates the inhibitory COOH-terminal tyrosine residue of src resulting in its activation.
  3. Tyrosine kinase-associated receptors - similar to tyrosine kinase receptors, but tyrosine kinase is not intrinsic to the receptor. Ligand binding causes the receptors to cluster, then recruits protein kinases from the cytosol (Cytokines such interleukins, interferons, and colony-stimulating factors)
  4. Receptor serine/threonine kinases - kinase activity on their cytoplasmic domains (Transforming growth factor)
  5. Receptor guanylyl cyclases - cytoplasmic domains that contain guanylatecyclase activity. Activation of these receptors increases cGMP. In this type of receptor there is no G-protein involvement
108
Q

Types of Intracellular targets

A

***drug must gain access to the cell by diffusion or by being
transported into the cell.
1. Regulation of intracellular enzymes.
2. Regulation of transcription. Steroid hormones bind an intracellular receptor. Dimerized hormone receptor complex then binds to DNA and regulates gene transcription
3. Structural proteins. Drugs like the vinca alkaloids bind to tubulin monomers and prevent the formation of microtubules. Drugs used in chemo

109
Q

What sx is characteristics of organophosphate poisioning?

A

Muscle weakness due to toxicity a BOTH nAChR (mm. sx) and mAChR

110
Q

Death from cholinesterase inhibitor poisoning is usually due to:

A

respiratory failure from combination of: bronchoconstriction, bronchorrhea, central respiratory depression, weakness or paralysis of respiratory muscles

111
Q

Organophosphate treatment:

A

An -oxime, ie pralidoxime (2-PAM)

112
Q

What reversible AChE inhbitior is used to reverse atropine OD?

A

Physostigmine

113
Q

what is used to counteract the muscarinic and CNS effects of organophosphate poisioning?

A

Atropine which binds mAChR outcompeting increased levels of ACh preventing overstim

114
Q

Signs of organophosphate poisoning?

A

SLUDGE BAM - salivation, lacrimation, urination, diaphoresis, GI motilitiy/diarrhea, emesis Bradycardia/ Bronchoconstriction/ Bowel movement Abdominal cramps/ Anorexia Miosis

115
Q

Muscarinic excess in parasympathetic system:

A

Bronchospasm, bronchorrhea, miosis, lacrimation, urination, diarrhea, bradycardia, vomiting, and salivation, sweating

116
Q

Nicotinic excess in sympathetic system:

A

hypotension (desensitization of receptors on sympathetic ganglia),
sweating (also direct muscarinic effect)

117
Q

Overstimulation of muscarinic and nicotinic receptors in the CNS:

A

Confusion, agitation, coma, respiratory failure, convulsions.

118
Q

Overstimulation of nicotinic receptors at the neuromuscular junction:

A

muscle weakness, paralysis, fasciculation - mm. involvement is give-away sign for organophosphate poisoing

Pharm (3 decks)

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