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Pharmacology Flashcards

1
Q

Pharmacokinetics

A

The effect of the body on the drug

ADME:
Absorption, distribution, metabolism, excretion

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2
Q

Pharmacodynamics

A

The effects of the drug on the body

Includes drug efficacy, drug potency, drug toxicity

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3
Q

Bioavailability (F)

A

Fraction of administered drug that reaches systemic circulation unchanged

For an IV dose, F = 100%

Orally F typically <100% due to incomplete absorption and first-pass metabolism

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4
Q

Volume of distribution Vd

A

Theoretical volume occupied by the total absorbed drug amount at the plasma concentration measured

Vd = amount of drug / plasma drug concentration

Low Vd: drug in Vd
Medium Vd: drug in ECF
High Vd: drug in all tissues including fat

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5
Q

Half life T1/2

A

Time required to change the amount of drug in the body by 1/2 during elimination

Property of ONLY first-order elimination

Drug infused at a constant rate takes 4-5 half lives to reach steady state

T1/2 = (0.693 x Vd) / Clearance (CL)

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6
Q

Clearance CL

A

The volume of plasma cleared of drug per unit time.

Clearance may be impaired with defects in cardiac, hepatic, or renal function

CL = rate of elimination / plasma drug concentration

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7
Q

Dosage calculation

A

Loading dose = (Cp (target concentration) x Vd ) / F
Maintenance dose = (Cp x CL x tau (dosage interval) ) / F

In renal or liver disease, maintenance dose decreases but loading dose is usually unchanged

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8
Q

Zero order elimination

A

Rate of elimination is constant regardless of drug concentration

Concentration decreases linearly w time

Ex: phenytoin, ethanol, aspirin

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9
Q

First order elimination

A

Rate of elimination is directly proportional to the drug concentration

Concentration decreases exponentially w time

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10
Q

Urine pH and drug elimination

A

Ionized species are trapped in urine and cleared quickly while neutral ones are often reabsorbed

Weak acids: aspirin, methotrexate, trapped in basic environment, add bicarb for overdose

Weak bases: amphetamines, trapped in acidic environment, add ammonium chloride for overdose

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11
Q

Drug metabolism

A

Phase I: reduction, oxidation, hydrolysis with cytochrome p450, usually yields slightly polar, water-soluble metabolites often still active

Phase II: conjugation (glucuronidation, acetylation, sulfation) usually yields very polar, inactive metabolites (renal excreted)

Geriatric patients often lose phase 1 before phase 2

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12
Q

Efficacy

A

Maximal effect a drug can produce

High efficacy drug classes are analgesic medications, antibiotics, antihistamines

Partial agonists often have less efficacy than full agonists

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13
Q

Potency

A

Amount of drug needed for a given effect

Increased potency usually means increased affinity for a certain receptor

Highly potent drugs include chemotherapeutic drugs, antihypertensives, and lipid lowering drugs

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14
Q

Competitive antagonist

A

No change in efficacy but decreases potency of original drug

Efficacy is overcomes by increasing the concentration of original agonist substrate

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15
Q

Noncompetitive antagonist/irreversible competitive antagonist

A

Decreases efficacy.

Cannot be overcome by increasing concentration of original agonist substrate

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16
Q

Partial agonist

A

Acts at the same site as full agonist, but with lower maximal efficacy.

Potency can vary compare to full agonist depending on concentration and type

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17
Q

Nicotinic Ach receptor

A

Ligand gated Na/K channels

Nn found in autonomic ganglia

Nm found in neuromuscular junction

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18
Q

Muscarinic Ach receptor

A

G protein coupled receptors that usually act through 2ndary messengers

5 subtypes: M1,2,3,45

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19
Q

Alpha1 receptor

A

Sympathetic

Increase vascular smooth muscle contraction
Increase pupillary dilator muscle contraction
Increase intestinal and blade sphincter muscle contraction

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20
Q

Alpha2 receptor

A

Sympathetic

Decrease sympathetic outflow
Decrease insulin release
Decrease lipolysis

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21
Q

Beta1 receptor

A

Sympathetic

Increase heart rate
Increase heart contractility
Increase renin release
Increase lipolysis

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22
Q

Beta2 receptor

A

Sympathetic

Vasodilation
Bronchodilation
Increase heart rate
Increase heart contractility
Increase insulin release
Decrease uterine tone
Increase aqueous humor production
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23
Q

M1

A

Parasympathetic

CNS
Enteric nervous system

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24
Q

M2

A

Parasympathetic

Decrease heart rate
Decrease contractility of atria

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25
M3
Parasympathetic Increase exocrine gland secretions Increase gut peristalsis Increase blade contraction Increase pupillary sphincter muscle contraction Ciliary muscle contraction for accomondation
26
D1
Dopamine Relaxes renal vascular smooth muscle
27
D2
Dopamine Modulates transmitter release, especially in brain
28
H1
Histamine Increase nasal and bronchial mucus production Increase vascular permeability
29
H2
Histamine Increase gastric acid secretion
30
V1
Vasopressin Increase vascular smooth muscle contraction
31
V2
Vasopressin Increase water permeability and reabsorption in the collecting tubules of kidney
32
Bethanechol
Cholinergic agonist Activates bowel and bladder smooth muscle, resistant to AChEsterase For postoperative ileus, neurogenic ileus, and urinary retention
33
Carbachol
Cholinergic agonist For glaucoma and relief of intraocular pressure
34
Pilocarpine
Cholinergic agonist Resistant to AChE Potent stimulator of sweat, tears, and saliva Treatment for open angle and close angle glaucoma
35
Neostigmine
Anti-AChE Increases ACh For posteroperative and neurogenic ileus and urinary retention, myasthenia gravis
36
Pyridostigmine
Anti-AChE Increase ACh For myasthenia gravis, does not penetrate CNS
37
Physostigmine
Anti-AChE Increase ACh Penetrates CNS, treats anticholinergic toxicity (atropine overdose)
38
Donepzil, rivastigmine
Anti-AChE Increase ACh For Alzheimer disease
39
AChE inhibitor poisoning
Too much cholinergics Often due to organophosphates, such as components of insecticides, that irreversibly inhibit AChE ``` DUMBBELSS: Diarrhea Urination Miosis Bronchospasm Bradycardia Excitation of skeletal muscle and CNS Lacrimination Sweating Salivation ``` Antidote: atropine (competitive inhibitor) + pralidoxinme (regenerates AChE if used early)
40
Atropine
Muscarinic antagonist Blocks DUMBBELSS Also used to treat bradycardia Toxicity: too much anticholinergic hot as hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter Can cause acute angle glaucoma in elderly
41
Benztropine
Muscarinic antagonist Used to treat Parkinsons
42
Ipratropium
Muscarinic antagonist Used to treat COPD and asthma
43
Oxybutynin
Muscarinic antagonist Used to reduce urinary urgency
44
Glycopyrrolate
Muscarinic antagonist Used to reduce airway secretions and prevent peptic ulcers
45
Epinephrine
Sympathomimetic Beta > alpha Treat anaphylaxis, open angle glaucoma, asthma, hypotension Alpha effects become predominate effect at high dose
46
Norepinephrine
Sympathomimetic Alpha1 > alpha2 > beta 1 Treat hypotension
47
Dopamine
Sympathomimetic D1=D2 > beta > alpha Treat unstable bradycardia, heart failure, shock
48
Dobutamine
Sympathomimetic B1 > B2,alpha Treat heart failure, for cardiac stress test
49
Phenylephrine
Sympathomimetic A1 > A2 Treat hypotension, rhinitis (decongestant)
50
Albuterol, salmeterol
Sympathomimetic B2 > B1 Asthma, COPD
51
Amphetamine
Indirect general sympathetic agonist, reuptake inhibitor, release stored catecholemines Treat narcolepsy, ADHD
52
Ephedrine
Indirect general sympathetic agonist, release stored catecholemines Treat nasal congestion, urinary incontinence, hypotension
53
Cocaine
Indirect general sympathetic agonist, reuptake inhibitor NEVER give beta blocker if cocaine intoxication is suspected
54
Clonidine
Sympatholytic (alpha2 agonist) Treat hypertenisve urgency, ADHD Toxicity: CNS depression, bradycardia, hypotension, respiratory depression
55
Methyldopa
Sympatholytic (alpha2 agonist) Treat hypertension in pregnancy (only one safe in pregnancy) Toxicity: hemolytic anemia, SLE-like symptoms
56
Phenoxybenzamine
Alpha blocker, irreversible Treat pheochromocytoma to prevent catechlolamine crisis
57
Phentolamine
Alpha blocker, reversible Give to pts on MAO inhibitor if they eat tyramine-containing food
58
Prazosin, tamsulosin
Alpha 1 blocker Treat urinary symptoms of BPH
59
Mirtazapine
Alpha 2 blocker Treat depression
60
Beta blockers
Decrease heart rate/contractility, resulting in decreased O2 consumption --> angina Decreases MI mortality Decreases AV conduction velocity --> prevent SVT Decrease cardiac output and renin secretion --> HTN Decreases aqueous humor secretion --> glaucoma (timolol) Toxicity: impotence, bradycardia, AV block, seizures, sedation Avoid in cocaine users B1 selective block: atenolol, metoprolol Non selective alpha block: propanolol Non selective alpha and beta block: labetalol, carvedilol

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