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Pharmacology > Pharmacokinetics and Autonomic Drugs > Flashcards

Pharmacokinetics and Autonomic Drugs Flashcards

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1
Q

What is Bioavailability

A

Bioavailability (F) = % drug administered that reaches systemic circulation unchanged

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2
Q

In what instances is Bioavailability (F) 100%

A

IV administration, and in kids: interosseous

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3
Q

What is Volume of Distribution (Vd)

A

Vd = amount of drug in body / [drug] in plasma

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4
Q

What can change Volume of Distribution (Vd)?

A

kidney and liver diseases can change the Vd of protein bound drugs

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5
Q

What is the equation for half-life?

A

t1/2 = 0.7xVd/CL

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6
Q

What is clearance (Cl)

A 
Clearance = rate of elimination / [drug] in plasma
Clearance = Vd x Ke (Ke= elimination constant)
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7
Q

What is Loading Dose

A

Loading Dose = Cp x Vd/F where Cp = target [drug] in plasma

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8
Q

What is Maintenance Dose and what causes it to decrease

A

Maintenance Dose = Cp x Cl/F where Cp = target [drug] in plasma
Decreases in liver and kidney diseases because of decreased clearance

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9
Q

What is Steady State?

A

Depends on half-life of drug.
Most drugs require 4-5 half-lifes to reach steady state.
Not effected by frequency or amount of dosing

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10
Q

What is the difference between Zero and First order elimination?

A

0 order = constant amount is eliminated
eg: start 100, 80, 60, 40, 20, 0
1st order = constant fraction is eliminated
eg: start 100, 50, 25, 12.5, 6.25 etc

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11
Q

Which drugs are Zero order?

A

“Zero PEAs for me”

Phenytoin, Ethanol, Aspirin

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12
Q

What are weak acid drugs, where do they get trapped and how do you treat overdose?

A

Aspirin, Methotrexate, Phenobarbital
Trapped in basic environments
Use bicarbonate to treat overdose by ionizing, and trapping in urine

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13
Q

What are weak base drugs, where do they get trapped and how do you treat overdose?

A

Amphetamines
Trapped in acidic environments
Use ammonium chloride to treat overdose and trap in urine

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14
Q

What are Phase 1 types of drug metabolism? Which enzyme do they require? What do they yield? What occurs in Geriatric patients?

A

Reduction, Oxidation, Hydrolysis
Require cytochrome P450
Yield slightly polar, water-soluble, usually active metabolites
Phase 1 is lost first in geriatric patients

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15
Q

What are Phase 2 types of drug metabolism? What do they yield?

A

Glucuronidation, Acetylation, Conjugation

Yield very polar, inactive metabolites which are renally excreted

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16
Q

What occurs in slow acetylators?

A

increased side effects of drugs due to slower metabolism

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17
Q

Receptor a1: what g-protein class, and what are its functions

A

Gq,

Increase contraction of: vascular SmM, pupillary dilator muscle (mydriasis), intestinal and bladder sphincter muscle

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18
Q

Receptor a2: what g-protein class, and what are its functions

A

Gi,
Decrease sympathetic outflow, insulin release, lipolysis
increase platelet aggregation

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19
Q

Receptor b1: what g-protein class, and what are its functions

A

Gs,

Increase heart rate, contractility, renin release, lipolysis

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20
Q

Receptor b2: what g-protein class, and what are its functions

A

Gs,
Vasodilation, bronchodilation
Increased heart rate, contractility, lipolysis, insulin release, aqueous humor production
Decreased uterine tone, ciliary muscle relaxation

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21
Q

Receptor M1: what g-protein class, and what are its functions

A

Gq,

CNS, enteric nervous system

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22
Q

Receptor M2: what g-protein class, and what are its functions

A

Gi,

decrease heart rate, contractility of atri

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23
Q

Receptor M3: what g-protein class, and what are its functions

A

Gq,
Increased exocrine gland secretion (lacrimal, gastric etc), gut peristalsis, contraction of bladder, bronchioles, pupillary sphincter muscle (miosis), ciliary muscle (acommodation)

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24
Q

Receptor D1: what g-protein class, and what are its functions

A

Gs,

relaxes renal vascular SmM

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25
Receptor D2: what g-protein class, and what are its functions
Gi, | Modulates transmitter release, especially in brain
26
Receptor H1: what g-protein class, and what are its functions
Gq, | increased nasal, bronchial mucus production, contraction of bronchioles, puritis, pain
27
Receptor H2: what g-protein class, and what are its functions
Gs, | Increased gastric acid secretion
28
Receptor V1: what g-protein class, and what are its functions
Gq, | Increased vascular SmM contraction
29
Receptor V2: what g-protein class, and what are its functions
Gs, | Increased H2O permeability, reabsorption in collecting tubules of kidney
30
Hemicholinium: Site of action,
Inhibits choline reuptake on presynaptic cholinergic neuron
31
Vesamicol: Site of action
Cholinergic neuron: Inhibits intracellular transportation of Acetyl-CoA and Choline via ChAT into secretory vessicle for assembly into ACh
32
Botulinum: site of action
Cholinergic neuron: Inhibits release of ACh into synaptic cleft
33
Metyrosine: Site of action
Noradrenergic neuron: inhibits conversion of tyrosine into dopa, therefore decreasing production of dopamine and NE
34
Reserpine: Site and mechanism of action
Noradrenergic neuron: irreversibly blocks VMAT (vesiclular monoamine transporter) so that NE, 5HT3, and Dopamine cannot enter secretory vesicles for exocytosis. They are degraded by MAO and COMT in the cytoplasm, and [monoamine] in the synapse is depeated, leading to depression
35
Guanethidine, Bretylium: site of action
inhibit release of NE into synapse
36
Amphetamine: site of action
increases release of NE into synase
37
Cocaine, TCAs, Amphetamines
inhibit reuptake of NE into presynaptic neuron
38
Bethanechol: Direct or Indirect agonist? Clinical application? Action?
Direct agonist (cholinomimetic) Application: Postoperative ileus, neurogenic ileus (constipation), urinary retention Action: (+) bowel and bladder SmM, resistant to AChE "BETHANy, CHOL me if you want to activate your bowels and bladder"
39
Carbachol: Direct or Indirect agonist? Clinical application? Action?
``` Direct agonist (cholinomimetic) Application: glaucoma, pupillary contraction, relief of intraocular pressure Action: "CARBon copy of ACh" ```
40
Pilocarpine: Direct or Indirect agonist? Clinical application? Action?
Direct agonist (cholinomimetic) Application: open-angle and closed-angle glaucoma Action: potent stimulator of sweat, tears, saliva. Contracts ciliary muscle of eye for open-angle, and pupillary sphinter for closed angle. resistant to AChE "Cry, Drool, Sweat on your PILOw"
41
Methacholine: Direct or Indirect agonist? Clinical application? Action?
Direct agonist (cholinomimetic) Application: challenge test for asthma Action: (+) M receptors in airway
42
Neostigmine: Direct or Indirect agonist? Clinical application? Action?
``` Indirect Agonist (anti-AChE) Application: same as Bethanechol (postoperative neurogenic ileus and urinary retention) + myasthenia gravis, reversal of neuromuscular junction blockade (postop) Action: increase endogenous ACh, "Neo CNS = No CNS penetration" ```
43
Pyridostigmine: Direct or Indirect agonist? Clinical application? Action?
``` Indirect agonist (anti-AChE) Application: Myasthenia gravis (long acting), does not penetrate CNS Action: same as neostigmine. Increase endogenous ACh so increase strength "pyRIDostiGMine gets RID of Myasthenia Gravis" ```
44
Edrophonium: Direct or Indirect agonist? Clinical application? Action?
``` Indirect agonist (anti-AChE) Application: diagnosis of myasthenia gravis (extremely short acting) Action: increases endogenous ACh ```
45
Physostigmine: Direct or Indirect agonist? Clinical application? Action?
``` Indirect agonist (anti-AChE) **do not confuse with pyridostigmine for myasthenia Application: Anticholinergic toxicity ( x BBB into CNS) Action: increase endogenous ACh **FOR ATROPINE OD "Physostigmine Phyxes atropine OD" ```
46
Donepezil: Direct or Indirect agonist? Clinical application? Action?
``` Indirect agonist (Anti-AChE) Application: Alzheimer's Action: increase endogenous ACh ```
47
Cholinesterase Inhibitor Poisoning: Causes, effects, antidote
Causes: organophosphates (Parathion) found in insecticides, which irreversibly (-) AChE Effects: Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal musc and cns, Lacrimation, Sweating, Salivation Antidote: atropine + pralidoxime (regenerates AChE)
48
Atropine, Homatropine, Tropicamide: Drug type, Organ system, Application
Muscarinic antagonist Eye Produce mydriasis and cycloplegia
49
Benztropine: Drug type, Organ system, Application
Muscarinic antagonist CNS Parkinsons "Park my Benz"
50
Scopolamine: Drug type, Organ system, Application
Muscarinic antagonist CNS + auditory nerve Motion sickness
51
Ipratropium, Tiotropium: Drug type, Organ system, Application
Muscarinic antagonist Respiratory COPD, Asthma "IPRAy i can breathe soon"
52
Oxybutynin: Drug type, Organ system, Application
Muscarinic antagonist Genitourinary Reduce urgency in mild cystitis and reduce bladder spasms
53
Glycopyrrolate: Drug type, Organ system, Application
Muscarinic antagonist GI, Respiratory Parenteral: preop for reducing airway secretions; Oral: drooling, peptic ulcer
54
Atropine: Drug type, Main Use, Action, Toxicity, Side Effects
Muscarinic antagonist Main use: bradycardia and ophthalmic Action: - increase pupil dilation and cycloplegia, - decrease airway secretions, stomach acid secretions, gut motility, bladder urgency in cystitis - BLOCKS DUMBBeLSS but not excitation of CNS and SkM because that is mediated by nicotinic receptors Toxicity: - increase body temp (since decr sweating), rapid pulse, dry mouth, dry flushed skin, cycloplegia, constipation, disorientation ("hot as a hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter") - acute-CLOSURE glaucoma in elderly due to mydriasis, urinary retention in men w/ BPH, and hyperthermia in infants - Jimson Weed
55
Epinephrine: Drug type, Receptor affinity, Application
Direct Sympathomimetic b > a, no affinity for D1 Application: anaplylaxis, open angle glaucoma, asthma, hypotension
56
Norepinephrine: Drug type, Receptor affinity, Application, Cardiovascular effects
Direct Sympathomimetic a > b1, no affinity for b2 or D1 Application: hypotension (but decrease renal perfusion) CV effects: a1 mediated increase in systolic and diastolic pressures due to vasoconstriction, incr MAP, leading to bradycardia
57
Isoproterenol: Drug type, Receptor affinity, Application, Cardiovascular effects
Direct Sympathomimetic b1 and 2, no affinity for a or D Application: Torsade de pointes (tachycardia decreases QT interval), bradyarrhythmias (but may worsen ischemia) CV effects: b2 mediated vasodilation leading to decreased MAP and increased HR through b1 reflex
58
Dopamine: Drug type, Receptor affinity, Application
Direct Sympathomimetic D1 at low dose, b1 and b2 at medium dose, a1 and a2 at high dose Application: Shock (renal perfusion), HF, inotropic and chronotropic
59
Dobutamine: Drug type, Receptor affinity, Application
Direct Sympathomimetic b1 >> b2 or a1, a2 Application: HF, cardiac stress testing, inotropic and chronotropic
60
Phenylephrine: Drug type, Receptor affinity, Application
Direct Sympathomimetic a1 > a2, no affinity for b or D1 Application: hypotension (vasoconstriction), occular procedures (mydriatic), rhinitis (decongestant)
61
Metaproterenol, Albuterol, salmeterol, terbutaline: Drug type, Receptor affinity, Application
Direct Sympathomimetic b2 >> b1, no affinity for a or D1 Application: - metaproterenol and albuterol for acute asthma - salmeterol for long-term asthma or COPD - terbutaline to reduce premature uterine contractions
62
Ritodrine: Drug type, Receptor affinity, Application
Direct Sympathomimetic b2 only Application: reduces premature uterine contractions
63
Amphetamine: Drug type, Mechanism, Application
Indirect Sympathomimetic releases stored catecholamines Application: narcolepsy, obesity, ADD
64
Ephedrine: Drug type, Mechanism, Application
Indirect Sympathomimetic releases stored catecholamines Application: Nasal decongestion, urinary incontinence, hypotension
65
Cocaine: Drug type, Mechanism, Application, Contraindication
Indirect Sympathomimetic Reuptake inhibitor Application: Vasoconstriction and local anesthesia Contraindication: Never give b-blocker if cocaine intoxication is suspected (lead to unopposed a1 activation, extreme htn)
66
Clonidine, a-methyldopa: Drug type, Mechanism, Application
Sympathoplegics Centrally acting a2-agonist, decrease central sympathetic outflow Application: HTN (especially w/ renal dz)
67
Phenoxybenzamine: Drug type, Application, Toxicity
Irreversible Nonselective a-blocker Pheochromocytoma -- used before removing tumor to irreversibly block a-receptors since it won't be overcome by the high levels of released catecholamines Toxicity: orthostatic hypotension, reflex tachycardia
68
Phentolamine: Drug type, Application
Reversible Nonselective a-blocker | For patients on MAO inhibitors who eat tyramine-containing foods (red wine, cheese, fish)
69
(Praz/Teraz/Doxaz/Tamsul)-osin: Drug type, Application, Toxicity
"-osin" = a1-selective blocker For htn, urinary retention in BPH Toxicity: first dose orthostatic hypotension, dizziness, headache
70
Mirtazapine: Drug type, Application, Toxicity
a2-selective blocker For depression Toxicity: sedation, increased serum cholesterol and appetite
71
(Acebut-, betax-, esm-, aten-, metopr-, propran-, tim-, pind-, labet-)-olol: Drug type, Application and effect, Toxicity, Use with caution in...
b-blockers Angina pectoris -- decrease HR, contractility, so less O2 consumption MI -- decrease mortality Hypertension -- decrease CO and renin secretion (because JGA cell b1 blockade!!) CHF -- slow progression of chronic failure Toxicity: impotence, exacerbation of asthma, cardiovasc (bradycardia, AV block, CHF), CNS (seizures, sedation, sleep alterations) Caution in diabetics because b2 receptors increase insulin release so inhibiting b will decrease insulin leading to hyperglycemia
72
b-blockers for SVT
metoprolol, esmolol (class II antiarrhythmic)
73
b-blocker for glaucoma
timolol | decrease secretion of aqueous humor
74
Name the b1-selective antagonists, and use
Acebutalol (partial agonist), Betaxolol, Esmolol (short acting), Atenolol, Metoprolol Advantageous in pts w/ comorbid pulmonary disease
75
Name the non-selective b antagonists
Propranolol, Timolol, Nadolol, Pindolol
76
Name the non-selective vasodilatory a- and b-antagonists
Carvedilol, Labetalol
77
Name the partial b-agonists
Pindolol and acebutalol Partial Agonist Pindolol Acebutalol (PAPA) note: pindolol is also non-selective antagonist, and acebutalol is b1 selective antagonist)

Pharmacology (12 decks)

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