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FirstAID > Pharmacology > Flashcards

Pharmacology Flashcards

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
Q

Symptoms of cholinesterase-inhibitor / Organophosphate Poisoning:

A
  • ->”DUMBBELSS”
  • Diarrhea
  • Urination
  • Miosis
  • Bronchospasm
  • Bradycardia
  • Excitation of skeletal muscle and CNS
  • Lacrimation
  • Sweating
  • Salivation
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26
Q

Antidote/Treatment of organophosphate/cholinesterase-inhibitor poisoning?

A

–> Atropine + Pralidoxime (generates active AChE)

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27
Q

Homatropine:

A
  • -> anti-choinergic (like atropine)
  • acts on eye
  • Causes:
  • mydriasis
  • cycloplegia (paralyzes ciliary muscle)
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28
Q

Tropicamide:

A
  • -> anti-choinergic (like atropine)
  • acts on eye
  • Causes:
  • mydriasis
  • cycloplegia (paralyzes ciliary muscle)
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29
Q

Benztropine:

A
  • anti-cholinergic
  • acts on CNS
  • treats Parksinon’s (improves tremor and rigidity from excess cholinergic activity; no effect on dopamine levels or bradykinesia)
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30
Q

Scopolamine:

A
  • anti-cholinergic
  • acts on CNS
  • Treats motion sickness (“want to vomit as I scope out the window of the moving car”)
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31
Q

Ipratropium:

A
  • anti-cholinergic
  • acts on respiratory system
  • Treats Asthma and COPD (“I Pray I can breathe soon!”)
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32
Q

Oxybutynin:

A
  • anti-cholinergic
  • acts on genitourinary system
  • reduces urgency in mild cystitis and reduces bladder spasms
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33
Q

Glycopyrrolate:

A
  • anti-cholinergic
  • acts on genitourinary system
  • reduces urgency in mild cystitis and reduces bladder spasms
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34
Q

Methscopolamine:

A
  • anti-cholinergic
  • acts on GI system
  • treats peptic ulcers
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35
Q

Propantheline:

A
  • anti-cholinergic
  • acts on GI system
  • treats peptic ulcers
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36
Q

Atropine:

  • mechanism?
  • uses?
  • effects on: eye, airway, stomach, gut, bladder?
A
  • 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
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37
Q

Atropine Toxicity:

A
  • 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)
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38
Q

Epinephrine:

  • acts on which receptors?
  • uses?
A

*acts on alpha1, alpha2, beta1, beta2

  • uses:
  • Anaphylactic shock
  • open angle Glaucoma
  • Asthma
  • Hypotension
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39
Q

Norepinephrine:

  • acts on which receptors?
  • uses?
A

-acts on alpha1 and alpha2, and less-so on beta1

  • Uses:
  • Hypotension
  • Septic shock
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40
Q

Isoproterenol:

  • acts on which receptors?
  • uses?
A
  • acts equally on beta1 and beta2

- treats AV block

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41
Q

Dopamine:

  • acts on which receptors?
  • uses?
A
  • 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)
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42
Q

Dobutamine:

  • acts on which receptors?
  • uses?
A

-mostly acts on Beta1, but also slightly on alpha1, alpha2, beta2

  • uses:
  • Heart failure
  • Cardiac stress testing
  • Cardiogenic shock
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43
Q

Phenylephrine:

  • acts on which receptors?
  • uses?
A

-mostly alpha 1, some alpha2

  • Applications:
  • pupillary dilation
  • vasoconstriction
  • nasal decongestion
  • good for stopping epistaxis!
44
Q

Metaproterenol:

  • acts on which receptors?
  • uses?
A
  • mostly beta-2 agonist; some beta 1

- treatment for acute asthma (like albuterol)

45
Q

Albuterol:

  • acts on which receptors?
  • uses?
A
  • mostly beta2 agonist; some beta1

- treatment of acute asthma

46
Q

Salmeterol:

  • acts on which receptors?
  • uses?
A
  • ->mostly Beta-2 agonist; some beta1

- ->long-term asthma treatment

47
Q

Terbutaline:

  • acts on which receptors?
  • uses?
A
  • ->mostly Beta-2 agonist; some beta-1

- ->Reduces premature uterine contractions (decreases uterine tone; so delays premature labor)

48
Q

Ritodrine:

  • acts on which receptors?
  • uses?
A
  • ->purely a Beta2 agonist

- used to reduce premature uterine contractions

49
Q

Amphetamines:

  • mechanism?
  • uses?
A

–>indirect sympathomimetic; stimulates release of stored catecholamines

  • Uses:
  • Narcolepsy
  • ADHD
  • Obesity
50
Q

Ephedrine:

  • mechanism?
  • uses?
A

–> indirect sympathomimetic; stimulates release of stored catecholamines

  • Uses:
  • nasal decongestion
  • urinary incontinence
  • hypotension
51
Q

Cocaine:

  • mechanism?
  • effects?
A

–>indirect sympathomimetic; inhibits reuptake of catecholamines

  • Effects:
  • Vasoconstriction
  • Local anesthesia
52
Q

Clonidine:

A
  • ->alpha-2-agonist
  • decreases BP
  • Uses:
  • Hypertension, especially with renal disease (b/c does not decrease blood flow to kidney)
53
Q

Methyldopa:

A
  • ->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
Q

Drug of choice for:

  • anaphylactic shock?
  • septic shock?
  • cardiogenic shock?
A
  • anaphylactic –> Epinephrine
  • septic –> Norepinephrine
  • cardiogenic –> Dobutamine
55
Q

Phenoxybenzamine:

  • mechanism?
  • uses?
  • toxicity?
A

Irreversible non-selective alpha-blocker

  • Use:
  • pheochromocytoma (give phenoxybenzamine before removing tumor)
  • Toxicity:
  • Orthostatic hypotension
  • reflex tachycardia
56
Q

Phentolamine:

  • mechanism?
  • use?
A

Reversible, non-selective alpha-blocker

  • Use:
  • give to pts on MAO inhibitors who eat tyrosine-containing foods
57
Q

drugs that end with “-zosin”

A

–> alpha-1-selective blockers

prazosin, terazosin, doxazosin

58
Q

Prazosin, Terazosin, Doxazosin:

  • mechanism?
  • use?
  • toxicity?
A

alpha-1-blockers

  • Uses:
  • HTN
  • urinary retention in BPH
  • Toxicities:
  • 1st dose orthostatic hypotension
  • dizziness
  • headache
59
Q

Mirtzazpine:

  • mechanism?
  • use?
  • toxicity?
A
  • alpha-2-blocker
  • Used in depression
  • Toxicity:
  • sedation
  • elevates serum cholesterol
  • increases appetite
60
Q

alpha-1 and alpha-2 blockage: effects on vaculature?

A

alpha-1-blockers –> vasodilation

alpha-2-blockers –> vasoconstriction

61
Q

Non-selective Beta-blockers:

A 
block B1=B2
"Please Try Not to Be (beta) Picky"
-Propranolol
-Timolol
-Nadalol
-Pindolol
62
Q

Beta-blockers that are partial Beta-agonists:

A
  • Pindolol (non-selective Beta-blocker)

- Acebutolol (Beta-1-blocker)

63
Q

Nonselective alpha and beta - blockers:

A
  • Carvedilol

- Labetalol

64
Q

Applications of Beta-Blockers:

A
  • 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
Q

Carvedilol

A

nonselective alpha AND beta blocker

–>vasodilatory

66
Q

Labetalol

A

nonselective alpha AND beta blocker

–>vasodilatory

67
Q

P-450 Inducers:

A

*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
Q

P-450 Inhibitors:

A

*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
Q

Sulfa Drugs:

A

“Popular FACTSSS”

  • Probenecid (gout)
  • Furosemide
  • Acetazolamide
  • Celecoxib
  • Thiazides
  • Sulfonamide antibiotics (ie SMX)
  • Sulfasalazine (UC and Crohn’s)
  • Sulonylureas (diabetes –> Glyburide)
70
Q

Drugs that may cause Dilated Cardiomyopathy?

A

–> Doxorubicin, Daunorubicin (anti-cancer drugs; generate free radicals–> intercalate DNA –> breaks DNA –> decreased replication)

71
Q

Drugs that may cause Agranulocytosis:

A

“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
Q

Drugs that may cause Aplastic Anemia:

A
  • Chloramphenicol
  • Benzenes
  • NSAIDs
  • Propylthiouracil
  • Methimazole
73
Q

Drugs that may cause Megaloblastic Anemia:

A

“having a Blast with PMS”

  • Phenytoin
  • Methotrexate
  • Sulfa drugs
74
Q

Drugs that may cause Pulmonary Fibrosis:

A

“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
Q

Drugs that may cause gynecomastia:

A

“Some Drugs Create Awesome Knockers”:

  • Spirinolactone
  • Digitalis
  • Cimetidine
  • Alcohol
  • Ketoconazole

*Also, Estrogens!

76
Q

Drugs that may cause Hypothyroidism:

A
  • Lithium
  • Amiodarone
  • Sulfonamides
77
Q

Drugs that may cause Gingivial Hyperplasia:

A
  • Phenytoin

- Verapamil (CCB)

78
Q

Drugs that may cause Photosensitivity:

A

“SAT for a Photo”:

  • Sulfonamides
  • Amiodarone
  • Tetracycline
79
Q

Drugs that may cause drug-induced lupus:

A

“SHIPP”

  • Sulfas
  • Hydralazine
  • Isoniazid
  • Procainamide
  • Phenytoin
80
Q

Drug that may cause tendonitis, tendon rupture, cartilage damage in kids:

A

–> Fluoroquinolones (FluoroquinoBONES!)

81
Q

Drugs that may cause Nephrotoxicity + Ototoxicity:

A
  • Cisplatin
  • Carbaplatin
  • Aminoglycosides
  • Loop diuretics
  • Vancomycin
82
Q

Fomepizole:

A

–>Antidote for Methanol/Ethylene glycol (antifreeze) toxicity

83
Q

Flumazenil

A

antidote for benzo toxicity

84
Q

Protamine

A

antidote for Heparine toxicity

85
Q

Aminocaproic acid

A

antidote for tPA, Streptokinase, Urokinase

86
Q

Dimercaprol

A

Treatment for lead poisoning

antidote for mercury, arsenic, gold toxicity

87
Q

Penicillamine

A

antidote for copper, arsenic, gold toxicity

88
Q

Deferoxamine

A

antidote for iron toxicity

89
Q

N-acetylcysteine:

A

antidote for acetaminophen toxicity (regenerates glutathione)

-AND-

mucolytic agent –> used to loosen mucous plugs in CF pts

90
Q

Methylene blue

A

antidote for methemoglobin toxicity

91
Q

Treatment for Cyanide poisoning?

A

First: Nitrites –> oxidize Hb to Met-Hb
Then: Thiosulfates –> renally excrete thiocyanate (thiosulfate bound to cyanide)

92
Q

Drugs that may cause Hypothyroidism:

A
  • Lithium
  • Amiodarone
  • Sulfonamides
93
Q

Drugs that may cause Gingivial Hyperplasia:

A
  • Phenytoin

- Verapamil (CCB)

94
Q

Drugs that may cause Photosensitivity:

A

“SAT for a Photo”:

  • Sulfonamides
  • Amiodarone
  • Tetracycline
95
Q

Drugs that may cause drug-induced lupus:

A

“SHIPP”

  • Sulfas
  • Hydralazine
  • Isoniazid
  • Procainamide
  • Phenytoin
96
Q

Drug that may cause tendonitis, tendon rupture, cartilage damage in kids:

A

–> Fluoroquinolones (FluoroquinoBONES!)

97
Q

Drugs that may cause Nephrotoxicity + Ototoxicity:

A
  • Cisplatin
  • Carbaplatin
  • Aminoglycosides
  • Loop diuretics
  • Vancomycin
98
Q

Fomepizole:

A

–>Antidote for Methanol/Ethylene glycol (antifreeze) toxicity

99
Q

Flumazenil

A

antidote for benzo toxicity

100
Q

Protamine

A

antidote for Heparine toxicity

101
Q

Aminocaproic acid

A

antidote for tPA, Streptokinase, Urokinase

102
Q

Dimercaprol

A

antidote for mercury, arsenic, gold toxicity

103
Q

Penicillamine

A

antidote for copper, arsenic, gold toxicity

104
Q

Deferoxamine

A

antidote for iron toxicity

105
Q

N-acetylcysteine:

A

antidote for acetaminophen toxicity (regenerates glutathione)

-AND-

mucolytic agent –> used to loosen mucous plugs in CF pts

106
Q

Methylene blue

A

antidote for methemoglobin toxicity

107
Q

Treatment for Cyanide poisoning?

A

First: Nitrites –> oxidize Hb to Met-Hb
Then: Thiosulfates –> renally excrete thiocyanate (thiosulfate bound to cyanide)

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