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Pharmacology Flashcards

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1
Q

How many half-lifes does it take for a drug infused at a constant rate to reach steady state?

A

–>4-5 half-lives

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2
Q

List 3 drugs with zero-order elimination?

A

“PEA”

  • Phenytoin
  • Ethanol
  • Aspirin
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3
Q

Phase 1 drug metabolism:

A

–>Involves cytochrome P-450

  • Reduction, Oxidation, Hydrolysis
  • Usually yields slightly polar, water-soluble metabolites (often still active)
  • lost first in geriatric patients
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4
Q

Phase 2 drug metabolism:

A

–>involves conjugation

  • “GAS”
  • Glucuronidation
  • Acetylation
  • Sulfation
  • Usually yileds very polar, inactive metabolites, that are renally excreted
  • Geriatric patients retain GAS (phase 2)!
  • pts who are slow acetylators –> slower rate of drug metabolism –> increased side effects from certain drugs
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5
Q

Efficacy:

A

proportional to Vmax

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6
Q

Potency:

A

inversely proportion to Km

–>same as affinity for receptor

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7
Q

Therapeutic Index (TI):

A

“TILE”

TI = LD50/ED50

  • LD50: median lethal dose
  • ED50: median effective dose
  • decreased TI –> more lethal
  • safer drugs have higher TI values
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8
Q

What type of receptors are Nicotinic ACh receptors?

A

–>Ligand-gated Na/K channels

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9
Q

What type of receptors are Muscarinic ACh receptors?

A

–> G-protein-coupled receptors; act through second messengers.

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10
Q

4 Direct cholinergic agonists:

A
  • Bethanochol
  • Carbachol
  • Pilocarcpine
  • Methacholine
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11
Q

6 Indirect cholinergic agonists = Anti-cholinesterases:

A
  • Neostigmine
  • Physostigmine
  • Pyridostigmine
  • Edrophonium
  • Echothiophate
  • Donepezil
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12
Q

Bethanechol:

  • mechanism?
  • action?
  • uses?
A

Direct cholinergic agonist

  • activates bowel and bladder smooth muscle
  • resistant to AChE
  • Uses:
  • postoperative neurogenic ileus and urinary retention
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13
Q

Carbachol:

  • mechanism?
  • uses?
A
  • direct cholinergic agonist
  • Treatment of:
  • gluacoma
  • pupillary contraction
  • relief of intraocular pressure
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14
Q

Pilocarpine:

A
  • direct cholinergic agonist
  • resistant to AChE
  • stimulates sweat, tears, saliva
  • contracts ciliary muscle of eye
  • contracts pupillary sphincter of eye
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15
Q

Methacholine:

A
  • direct cholinergic agonist
  • stimulates muscarinic receptors in airway when inhaled (causing bronchoconstriction)

*Used as challenge test for asthma diagnosis

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16
Q

Neostigmine:

A
  • indirect cholinergic agonist = anti-Cholinesterase
  • increases endogenous ACh
  • NO CNS penetration
  • Uses:
  • postoperative and neurogenic ileus and urinary retention
  • myasthenia gravis
  • reverses neuromuscular junction blockade (post-operatively)
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17
Q

Pyridostigmine:

A
  • indirect cholinergic agonist = anti-cholinesterase
  • increases endogenous ACh
  • NO CNS penetration
  • Use:
  • Myasthenia Gravis (“gets RID of myasthenia gravis!”) (trtment b/c it’s long-acting)
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18
Q

Edrophonium:

A
  • indirect cholinergic agonist = anti-cholinesterase
  • increases endogenous ACh
  • Use:
  • Dx of Myasthenia Gravis (b/c it’s really short-acting)
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19
Q

Physostigmine:

A
  • indirect cholinergic agonist = anti-cholinesterase
  • increases endogenous ACh
  • Uses:
  • Atropine overdoes (“Phyxes atropine overdose”)
  • Glaucoma (b/c can cross BBB, penetrate CNS)
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20
Q

Echothiophate:

A
  • indirect cholinergic agonist = anti-cholinesterase
  • increase endogenous ACh
  • treats Glaucoma
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21
Q

Donepezil:

A
  • indirect cholinergic agonist = anti-cholinesterase
  • increases endogenous ACh
  • treats Alzheimer’s
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22
Q

Which cholinomimetic agents (cholinergic agonists) can be used to treat glaucoma?

A

Direct: Carbachol and Pilocarpine
Indirect: Physostigmine and Echothiophate

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23
Q

Pralidoxime:

A
  • ->treatment of cholinesterase-inhibitor poisoning (too much ACh)
  • ->action = regenerates AChE
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24
Q

Parathion:

A

–>insecticide = organophosphate = irreversible cholinesterase-inhibitor

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25
Symptoms of cholinesterase-inhibitor / Organophosphate Poisoning:
- ->"DUMBBELSS" - Diarrhea - Urination - Miosis - Bronchospasm - Bradycardia - Excitation of skeletal muscle and CNS - Lacrimation - Sweating - Salivation
26
Antidote/Treatment of organophosphate/cholinesterase-inhibitor poisoning?
--> Atropine + Pralidoxime (generates active AChE)
27
Homatropine:
- -> anti-choinergic (like atropine) - acts on eye * Causes: - mydriasis - cycloplegia (paralyzes ciliary muscle)
28
Tropicamide:
- -> anti-choinergic (like atropine) - acts on eye * Causes: - mydriasis - cycloplegia (paralyzes ciliary muscle)
29
Benztropine:
- anti-cholinergic - acts on CNS - treats Parksinon's (improves tremor and rigidity from excess cholinergic activity; no effect on dopamine levels or bradykinesia)
30
Scopolamine:
- anti-cholinergic - acts on CNS - Treats motion sickness ("want to vomit as I scope out the window of the moving car")
31
Ipratropium:
- anti-cholinergic - acts on respiratory system - Treats Asthma and COPD ("I Pray I can breathe soon!")
32
Oxybutynin:
- anti-cholinergic - acts on genitourinary system - reduces urgency in mild cystitis and reduces bladder spasms
33
Glycopyrrolate:
- anti-cholinergic - acts on genitourinary system - reduces urgency in mild cystitis and reduces bladder spasms
34
Methscopolamine:
- anti-cholinergic - acts on GI system - treats peptic ulcers
35
Propantheline:
- anti-cholinergic - acts on GI system - treats peptic ulcers
36
Atropine: - mechanism? - uses? - effects on: eye, airway, stomach, gut, bladder?
* anti-cholinergic * Uses: - treats bradycardia (like from an inferior MI) - ophthalmic applications (produces mydriasis and cycloplegia) - Blocks "DUMBELSS" (anti-cholinesterase/organophosphate poisoning) * Effects on: - Eyes --> mydriasis, cycloplegia - Airway --> decreases secretions - Stomach --> decreases acid secretions - Gut --> decreases motility - Bladder --> decreases urgency in cystitis
37
Atropine Toxicity:
* Hot as a hare (increased body temp) * Dry as a bone (decreased sweating, dry mouth, dry skin) * Red as a beet (flushed skin) * Blind as a bat (cycloplegia; and can cause acute angle-closure glaucoma in elderly) * Mad as a hatter (disorientation) * Bloated as a toad (constipation; also, urinary retention in men with prostatic hyperplasia)
38
Epinephrine: - acts on which receptors? - uses?
*acts on alpha1, alpha2, beta1, beta2 * uses: - Anaphylactic shock - open angle Glaucoma - Asthma - Hypotension
39
Norepinephrine: - acts on which receptors? - uses?
-acts on alpha1 and alpha2, and less-so on beta1 * Uses: - Hypotension - Septic shock
40
Isoproterenol: - acts on which receptors? - uses?
- acts equally on beta1 and beta2 | - treats AV block
41
Dopamine: - acts on which receptors? - uses?
* Effects are dose-dependent! - High Doses --> acts on alpha1 and alpha2 - Medium Doses --> acts on beta1 > beta2 - Low Dose --> acts on D1 * Uses: - increases renal perfusion in shock and heart failure - Inotropic (stimulates contractions) and Chronotropic (changes heart rate)
42
Dobutamine: - acts on which receptors? - uses?
-mostly acts on Beta1, but also slightly on alpha1, alpha2, beta2 * uses: - Heart failure - Cardiac stress testing - Cardiogenic shock
43
Phenylephrine: - acts on which receptors? - uses?
-mostly alpha 1, some alpha2 * Applications: - pupillary dilation - vasoconstriction - nasal decongestion - good for stopping epistaxis!
44
Metaproterenol: - acts on which receptors? - uses?
- mostly beta-2 agonist; some beta 1 | - treatment for acute asthma (like albuterol)
45
Albuterol: - acts on which receptors? - uses?
- mostly beta2 agonist; some beta1 | - treatment of acute asthma
46
Salmeterol: - acts on which receptors? - uses?
- ->mostly Beta-2 agonist; some beta1 | - ->long-term asthma treatment
47
Terbutaline: - acts on which receptors? - uses?
- ->mostly Beta-2 agonist; some beta-1 | - ->Reduces premature uterine contractions (decreases uterine tone; so delays premature labor)
48
Ritodrine: - acts on which receptors? - uses?
- ->purely a Beta2 agonist | - used to reduce premature uterine contractions
49
Amphetamines: - mechanism? - uses?
-->indirect sympathomimetic; stimulates release of stored catecholamines * Uses: - Narcolepsy - ADHD - Obesity
50
Ephedrine: - mechanism? - uses?
--> indirect sympathomimetic; stimulates release of stored catecholamines * Uses: - nasal decongestion - urinary incontinence - hypotension
51
Cocaine: - mechanism? - effects?
-->indirect sympathomimetic; inhibits reuptake of catecholamines * Effects: - Vasoconstriction - Local anesthesia
52
Clonidine:
- ->alpha-2-agonist - decreases BP * Uses: - Hypertension, especially with renal disease (b/c does not decrease blood flow to kidney)
53
Methyldopa:
- ->alpha-2-agonist - decreases BP *Treats HTN, especially with renal disease; b/c doesn't decrease blood flow to kidney ***can use methyldopa to treat HTN in pregnancy
54
Drug of choice for: - anaphylactic shock? - septic shock? - cardiogenic shock?
* anaphylactic --> Epinephrine * septic --> Norepinephrine * cardiogenic --> Dobutamine
55
Phenoxybenzamine: - mechanism? - uses? - toxicity?
Irreversible non-selective alpha-blocker * Use: - pheochromocytoma (give phenoxybenzamine before removing tumor) * Toxicity: - Orthostatic hypotension - reflex tachycardia
56
Phentolamine: - mechanism? - use?
Reversible, non-selective alpha-blocker * Use: - give to pts on MAO inhibitors who eat tyrosine-containing foods
57
drugs that end with "-zosin"
--> alpha-1-selective blockers | prazosin, terazosin, doxazosin
58
Prazosin, Terazosin, Doxazosin: - mechanism? - use? - toxicity?
alpha-1-blockers * Uses: - HTN - urinary retention in BPH * Toxicities: - 1st dose orthostatic hypotension - dizziness - headache
59
Mirtzazpine: - mechanism? - use? - toxicity?
* alpha-2-blocker * Used in depression * Toxicity: - sedation - elevates serum cholesterol - increases appetite
60
alpha-1 and alpha-2 blockage: effects on vaculature?
alpha-1-blockers --> vasodilation | alpha-2-blockers --> vasoconstriction
61
Non-selective Beta-blockers:
``` block B1=B2 "Please Try Not to Be (beta) Picky" -Propranolol -Timolol -Nadalol -Pindolol ```
62
Beta-blockers that are partial Beta-agonists:
- Pindolol (non-selective Beta-blocker) | - Acebutolol (Beta-1-blocker)
63
Nonselective alpha and beta - blockers:
- Carvedilol | - Labetalol
64
Applications of Beta-Blockers:
- HTN: decrease CO, decrease renin secretion (Beta-receptor blockade on JGA cells) - Angina pectoris: decrease HR and contractility; so, decrease O2 consumption of myocardium - MI: decrease mortality - SVT (Propranolol and Esmolol): decrease AV conduction velocity (class II antiarrhythmics) - CHF: slows progression - Glaucoma (Timolol, Betaxolol): decreases secretion of aqueous humor
65
Carvedilol
nonselective alpha AND beta blocker | -->vasodilatory
66
Labetalol
nonselective alpha AND beta blocker | -->vasodilatory
67
P-450 Inducers:
*Inducers--> increase metabolism rate; so decrease effect of other drugs "Queen Barb Steals Phenphen and Refuses Greasy Carbs Chronically" - Quinidine - Barbiturates - St John's wort - Phenytoin - Rifampin - Griseofulvin - Carbamazepine - Chronic alcohol
68
P-450 Inhibitors:
*Inhibitors--> slow metabolism rate; so increase toxicity of other drugs "MAGIC RACKS" - Macrolides - Amiodarone - Grapefruit juice - Isoniazid - Cimetidine - Ritonavir - Acute alcohol - Ciprofloxacin - Ketoconazole - Sulfonamides
69
Sulfa Drugs:
"Popular FACTSSS" - Probenecid (gout) - Furosemide - Acetazolamide - Celecoxib - Thiazides - Sulfonamide antibiotics (ie SMX) - Sulfasalazine (UC and Crohn's) - Sulonylureas (diabetes --> Glyburide)
70
Drugs that may cause Dilated Cardiomyopathy?
--> Doxorubicin, Daunorubicin (anti-cancer drugs; generate free radicals--> intercalate DNA --> breaks DNA --> decreased replication)
71
Drugs that may cause Agranulocytosis:
"Agranulocytosis Could Certainly Cause Pretty Major Damage) - Clozapine (atypical antipsychotic) - Carbamazepine (anti-epileptic) - Colchicine (gout) - Propylthioruracil (Graves) - Methimazole (Graves) - Dapsone (anti-bacterial, used to treat Mycobacterium leprae)
72
Drugs that may cause Aplastic Anemia:
- Chloramphenicol - Benzenes - NSAIDs - Propylthiouracil - Methimazole
73
Drugs that may cause Megaloblastic Anemia:
"having a Blast with PMS" - Phenytoin - Methotrexate - Sulfa drugs
74
Drugs that may cause Pulmonary Fibrosis:
"BAB" - Bleomycin (antitumor antibiotic; trtmnt for testicular cancer) - Amiodarone (Class III antiarrhythmic) - Busulfan (alkylating agent; trtmnt for CML and to prepare pt before BM transplant)
75
Drugs that may cause gynecomastia:
"Some Drugs Create Awesome Knockers": - Spirinolactone - Digitalis - Cimetidine - Alcohol - Ketoconazole *Also, Estrogens!
76
Drugs that may cause Hypothyroidism:
- Lithium - Amiodarone - Sulfonamides
77
Drugs that may cause Gingivial Hyperplasia:
- Phenytoin | - Verapamil (CCB)
78
Drugs that may cause Photosensitivity:
"SAT for a Photo": - Sulfonamides - Amiodarone - Tetracycline
79
Drugs that may cause drug-induced lupus:
"SHIPP" - Sulfas - Hydralazine - Isoniazid - Procainamide - Phenytoin
80
Drug that may cause tendonitis, tendon rupture, cartilage damage in kids:
--> Fluoroquinolones (FluoroquinoBONES!)
81
Drugs that may cause Nephrotoxicity + Ototoxicity:
- Cisplatin - Carbaplatin - Aminoglycosides - Loop diuretics - Vancomycin
82
Fomepizole:
-->Antidote for Methanol/Ethylene glycol (antifreeze) toxicity
83
Flumazenil
antidote for benzo toxicity
84
Protamine
antidote for Heparine toxicity
85
Aminocaproic acid
antidote for tPA, Streptokinase, Urokinase
86
Dimercaprol
Treatment for lead poisoning | antidote for mercury, arsenic, gold toxicity
87
Penicillamine
antidote for copper, arsenic, gold toxicity
88
Deferoxamine
antidote for iron toxicity
89
N-acetylcysteine:
antidote for acetaminophen toxicity (regenerates glutathione) -AND- mucolytic agent --> used to loosen mucous plugs in CF pts
90
Methylene blue
antidote for methemoglobin toxicity
91
Treatment for Cyanide poisoning?
First: Nitrites --> oxidize Hb to Met-Hb Then: Thiosulfates --> renally excrete thiocyanate (thiosulfate bound to cyanide)
92
Drugs that may cause Hypothyroidism:
- Lithium - Amiodarone - Sulfonamides
93
Drugs that may cause Gingivial Hyperplasia:
- Phenytoin | - Verapamil (CCB)
94
Drugs that may cause Photosensitivity:
"SAT for a Photo": - Sulfonamides - Amiodarone - Tetracycline
95
Drugs that may cause drug-induced lupus:
"SHIPP" - Sulfas - Hydralazine - Isoniazid - Procainamide - Phenytoin
96
Drug that may cause tendonitis, tendon rupture, cartilage damage in kids:
--> Fluoroquinolones (FluoroquinoBONES!)
97
Drugs that may cause Nephrotoxicity + Ototoxicity:
- Cisplatin - Carbaplatin - Aminoglycosides - Loop diuretics - Vancomycin
98
Fomepizole:
-->Antidote for Methanol/Ethylene glycol (antifreeze) toxicity
99
Flumazenil
antidote for benzo toxicity
100
Protamine
antidote for Heparine toxicity
101
Aminocaproic acid
antidote for tPA, Streptokinase, Urokinase
102
Dimercaprol
antidote for mercury, arsenic, gold toxicity
103
Penicillamine
antidote for copper, arsenic, gold toxicity
104
Deferoxamine
antidote for iron toxicity
105
N-acetylcysteine:
antidote for acetaminophen toxicity (regenerates glutathione) -AND- mucolytic agent --> used to loosen mucous plugs in CF pts
106
Methylene blue
antidote for methemoglobin toxicity
107
Treatment for Cyanide poisoning?
First: Nitrites --> oxidize Hb to Met-Hb Then: Thiosulfates --> renally excrete thiocyanate (thiosulfate bound to cyanide)

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