firstaid - pharm(1) Flashcards

1
Q

Cholinomimetics (direct)

A

Bethanechol
Carbachol
Pilocarpine
Methacholine

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2
Q

Bethanechol

A

activates bowel & bladder

postoperative ileus/neurogenic ileus, urinary retention treatment

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3
Q

Carbachol

A

carbon copy of Ach
glaucoma, relief of intraocular pressure
pupillary contraction

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4
Q

Pilocarpine

A

Stimulates sweat, tears, saliva
Open and close angle glaucoma

Resistant to acetylcholinesterase (AChE)

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5
Q

Methacholine

A

challenge test for ASTHMA

stimulates MUSCARINIC receptors in airway

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6
Q

Cholinomimetics (indirect) - ANTIcholinesterase

A
Neostigmine
Pyridostigmine
Edrophonium
Physostigmine
Donepezil
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7
Q

Neostigmine

A

Myasthenia gravis
postoperative/neurogenic ileus
urinary retention

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8
Q

Pyridostigmine

A
Myasthenia gravis (long acting)
does NOT penetrate CNS
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9
Q

Edrophonium

A
Myasthenia gravis (diagnosis) -- SHORT acting
Symptoms improve (proximal weakness - problems getting up from a chair, walking up stairs, eye drooping)
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10
Q

Physostigmine

A

Treats anticholinergic toxicity (reverse atropine toxicity) - crosses CNS

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11
Q

Donepezil

A

Alzheimer’s disease

Helps symptoms but does not cure disease

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12
Q

Side effects of ALL cholinomimetics

A

exacerbation of COPD, asthma, peptic ulcers

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13
Q

Cholinesterase inhibitor poisoning

too much acetylcholinesterase inhibitors

A

organophosphates poisoning (insecticides)

DUMBBELSS
diarrhea
urination
miosis
bronchospasm
bradycardia
excitation of skeletal muscle/CNS
lacrimation
sweating
salivation
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14
Q

Reveral of cholinesterase inhibitor poisoning

A

ATROPINE + pralidoxime

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15
Q

Reversal of atropine poisoning

atropine is muscarinic antagonist - decreases actions of Ach

A

Physostigmine (cholinesterase inhibitor to INCREASE Ach)

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16
Q

Muscarinic antagonists

A
Benztropine
Scopolamine
Ipratropium
Oxybutynin
Glycopyrrolate
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17
Q

Atropine

A

Mydriasis (risk of acute angle closure glaucoma)

Cycloplegia (loss of accomodation)

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18
Q

Benztropine

A

treats Parkinson’s disease

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19
Q

Scopolamine

A

Motion sickness

muscarinic cholinergic ANTAGONIST

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20
Q

Ipratropium mechanism & uses

A

Asthma & COPD
muscarinic cholinergic receptor ANATAGONIST

Blocks action of Ach on muscarinic receptors (Ach released when vagal nerve stimulated –> parasympathetics –> bronchoconstriction)

Ipratropium is beta2 agonist – bronchodilation

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21
Q

Oxybutynin

A

anticholinergic

decrease urgency (cystitis)
decrease bladder spasms due to antimuscarinic action to smooth muscle cells
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22
Q

Glycopyrrolate

A

decrease mucus secretion in airway
decrease drooling
decrease gastric secretion (peptic ulcer)

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23
Q

Atropine: actions

A

muscarinic antagonist
blocks DUMBBeLLS

increase pupil dilation, cycloplegia
decrease secretions
decrease acid secretion
decrease motility
decrease urgency in cystitis

skeletal m. and CNS excitation mediated by nicotinic receptors (not affected by atropine)

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24
Q

Atropine toxicity: symptoms

A

increase body temperature (decrease sweating)
dry, flushed skin (peripheral vasodilation bc of no sweating)
cycloplegia (loss of accomodation)
acute angle closure glaucoma (in elderly)
urinary retention (old men w/ BPH)
hyperthermia (infants)

“hot, dry, red, blind, mad”

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25
Q

Sympathomimetics (direct)

A
Epinephrine
Norepinephrine
Isoproterenol
Dopamine
Dobutamine
Phenylephrine
Albuterol, Salmeterol, Terbutaline
Ritodrine
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26
Q

Epinephrine

A

alpha 1&2, beta 1&2

Indication:
anaphylaxis, glaucoma (open)
asthma
hypotension

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27
Q

Norepinephrine

A

alpha 1&2, beta 1
NO beta 2

Indication:
hypotension
(but DECREASE renal perfusion - bad!)

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28
Q

Isoproterenol

A

beta 1&2

Indication:
torsade de pointes
bradyarrhythmias (but worsens ischemia)

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29
Q

Dopamine

A

high dose - alpha 1&2
medium dose - beta 1&2
low dose - D1

Indications:

a) SHOCK (renal perfusion - raises BP)
b) Heart failure
c) Ionotropic (heart contraction) & chronotropic (heart rate)

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30
Q

Dobutamine

A

beta 1 agonist MAINLY
some alpha 1&2 (inotropic & chronotropic)

Indication:
HEART FAILURE

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31
Q

Phenylephrine

A

alpha 1&2

Actions:
Hypotension (vasoconstrictor)
Mydriasis (ocular procedures)
Decongestant (rhinitis)

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32
Q

Albuterol
Salmeterol
Terbutaline

A

beta 2 agonist MAINLY
some beta 1

metaproterenol & albuterol = acute asthma
salmeterol = long term asthma/COPD
terbutaline = prevent premature uterine contractions

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33
Q

Ritodrine

A

beta 2 agonist

reduce premature uterine contractions

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34
Q

Sympathomimetics (indirect)

A

Increase catecholamine release or decrease reuptake

Amphetamine
Ephedrine
Cocaine

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35
Q

Amphetamine

A

release stored catecholamines

narcolepsy
obesity
ADHD

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36
Q

Ephedrine

A

releases stored catecholamines

nasal decongestant
urinary incontinence
hypotension

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37
Q

Cocaine

A

catecholamine reuptake inhibitor

vasoconstriction
local anesthesia

*never give beta blockers if cocaine intoxication suspected (unopposed alpha 1 activation –> severe HTN)

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38
Q

Clonidine

alpha-methyldopa

A

Sympathoplegics

alpha-2 agonist
decrease sympathetic outflow

HTN (good for renal failure pts. bc it doesn’t compromise blood flow to kidneys)

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39
Q

alpha blockers (nonselective)

A

phenoxybenzamine

phentolamine

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40
Q

phenoxybenzamine (irreversible)

A

nonselective alpha adrenergic ANTAGONIST
pheochromocytoma

toxicity: orthostatic hypotension, reflex tachycardia

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41
Q

phentolamine (reversible)

A

treats patients on MAO inhibitors that eat tyramine-containing foods

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42
Q

alpha 1 selective inhibitors

A

“-osin” (prazosin)

HTN
urinary retention (BPH)
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43
Q

alpha 2 selective inhibtors

A

mirtazapine (increase outflow of sympathetics)

Rx for: depression

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44
Q

Beta blockers (selectivity)

A

“-olol”

A-M are beta1 selective antagonists
N-Z are nonselective beta antagonists

beta 1 selective prefered for patients w/ comorbid PULMONARY disease (beta 2 antagonists causes bronchoconstriction)

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45
Q

Beta blocker: angina pectoris

A

Decrease HR and contractility –> decrease O2 consumption

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46
Q

Beta blocker: MI

A

decrease mortality

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47
Q

Beta blocker: SVT (metoprolol, esmolol)

A

Metoprolol, Esmolol

Decrease AV conduction velocity (class II antiarrhythmic)

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48
Q

Beta blocker: HTN

A

Decrease CO

Decrease renin secretion (B1 receptor block on JGA cells)

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49
Q

Beta blocker: CHF

A

Slows progression of chronic failure

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50
Q

Beta blocker: Glaucoma

A

Timolol

Decrease secretion of aqueous humor

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51
Q

Nonselective alpha&beta antagonists

A

Carvedilol

Labetalol

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52
Q

Beta blockers w/ PARTIAL beta-agonistic activity (intrinsic sympathomimetic activity)

A

Pindolol

Acebutolol

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53
Q

Toxicity of B-blockers

A

a) Impotence (smooth muscle relaxation)
b) Exacerbation of asthma (B2 bronchodilation inhibited)
c) Bradycardia, AV block, CHF
d) Seizures, sedation, sleep alterations

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54
Q

B-blockers used w/ diabetics

A

Blunt symptoms of hypoglycemia – use w/ caution!

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55
Q

P450 inducers

A
Modafinil
Barbiturates
St. John's wort
Phenytoin
Rifampin
Griseofulvin
Carbamazepine
Chronic alcohol use
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56
Q

P450 inhibitors

A
Quinidine
Ciprofloxacin
Isoniazid
Grapefruit juice
Acute alcohol use
Erythromycin
Indinavir
Cimetidine
Sulfonamides
Ketoconazole
Amiodarone
Macrolides (some)
Gemfibrozil
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57
Q

Sulfa drugs (8)

A
Probenecid
Furosemide
Acetazolamide
Celecoxib
Thiazides
Sulfonamide antibiotics
Sulfasalazine
Sulfonylureas
Sulfa allergies:
Stevens-Johnson
UTI
pruritic rash, urticaria (hives)
hemolytic anemia, thrombocytopenia, agranulocytosis
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58
Q

-navir

A

protease inhibitor

Saquinavir

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59
Q

-triptan

A

5-HT 1B/1D agonist

Sumatriptan

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60
Q

-ane

A

Inhalational general anesthetic

Halothane

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61
Q

-caine

A

Local anesthetic

Lidocaine

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62
Q

-operidol

A

butyrphenone (neuroleptic)

Haloperidol

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63
Q

-azine

A

Phenothiazine (neuroleptic, antiemetic)

Chlorpromazine

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64
Q

-barbital

A

Barbituate

Phenobarbital

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65
Q

-zolam

A

BENZO

Alprazolam

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66
Q

-azepam

A

BENZO

Diazepam

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67
Q

-etine

A

SSRI

Fluoxetine – side effect: sexual dysfunction

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68
Q

-ipramine

A

TCA

Imipramine

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69
Q

-triptyline

A

TCA

Amitriptyline

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70
Q

-olol

A

b-antagonist

Propranolol

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71
Q

-terol

A

b2 agonist

Albuterol

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72
Q

-zosin

A

a1 antagonist

Prazosin

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73
Q

-oxin

A

Cardiac glycoside (inotropic)

Digoxin

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74
Q

-pril

A

Captopril

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75
Q

-afil

A

Erectile dysfunction

Sildenafil

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76
Q

-tropin

A

Pituitary hormone

Somatotropin

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77
Q

-tidine

A

H2 antagnoist

Cimetidine

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78
Q

Antidote: acetaminophen

A

N-acetylcysteine (replenishes glutathione)

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79
Q

Antidote: salicylates

A

NaHCO3 (alkalinize urine)

Dialysis

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80
Q

Antidote: amphetamines (basic)

A

NH4Cl (acidify urine)

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81
Q

Antidote: Acetylcholinesterase inhibitors, organophosphates

TOO MUCH ACH!

A

Atropine

Pralidoxime

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82
Q
Antidote: Antimuscarinic
Anticholinergic agents (eg. Atropine toxicity)
A

Physostigmine salicylate

Control hyperthermia

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83
Q

Antidote: B-blockers

A

Glucagon

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84
Q

Antidote: Digitalis

A

Normalize K+
Lidocaine
Anti-dig Fab fragments
Mg2+

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85
Q

Antidote: Iron

A

DeFEroxamine

DeFErasirox

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86
Q

Antidote: Lead

A

CaEDTA
Dimercaprol
Succimer
Penicillamine

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87
Q

Antidote: Mercury, arsenic, gold

A

Dimercaprol

Succimer

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88
Q

Antidote: Copper, arsenic, gold

A

Penicillamine

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89
Q

Antidote: Cyanide

A

Nitrite + thiosulfate

Hydroxocobalamin

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90
Q

Antidote: Methemoglobin

A

Methylene blue

Vitamin C

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91
Q

Antidote: Carbon monoxide

A

100% O2

Hyperbaric O2

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92
Q

Antidote: Methanol, ethylene glycol (antifreeze)

A

Fomepizole > ethanol

Dialysis

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93
Q

Antidote: Opioids

A

Naloxone

Naltrexone

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94
Q

Antidote: Benzodiazepines

A

Flumazenil

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95
Q

Antidote: TCAs

A

NaHCO3 (plasma alkalinization)

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96
Q

Antidote: Heparin

A

Protamine

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97
Q

Antidote: Warfarin

A

Vitamin K

Fresh frozen plasma

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98
Q

Antidote: tPA, streptokinase, urokinase

A

Aminocaproic acid

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99
Q

Antidote: Theophylline

A

B-blocker

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100
Q

G-protein linked 2nd messengers (5)

A
Sympathethic
Parasympathetic
Dopamine
Histamine
Vasopressin
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101
Q

Sympathethic

A

a1 - q
a2 - i
b1 - s
b2 - s

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102
Q

a1 receptor (3)

A

a) Increase vascular smooth muscle contraction
b) Increase pupillary dilatory muscle contraction (mydriasis – dilate)
c) Increase intestinal & bladder sphincter muscle contraction

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103
Q

a2 receptor (4)

A

a) DECREASE sympathetic outflow
b) DECREASE insulin release
c) DECREASE lipolysis
d) Increase platelet aggregation*

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104
Q

b1 receptor (4)

A

a) Increase HR
b) Increase contractility
c) Increase renin release
d) Increase lipolysis

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105
Q

b2 receptor (7)

A

a) Vasodilation
b) Bronchodilation
c) Increase HR, contractility; Increase lipolysis (similar to b1 receptor actions)
d) INCREASE insulin release
e) DECREASE uterine tone (delay childbirth) - tocolysis
f) Ciliary muscle relaxation
g) Increase aqueous humor production

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106
Q

Parasympathetic

A

M1 - q
M2 - i
M3 - q

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107
Q

M1 receptor

A

CNS

Enteric nervous system

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108
Q

M2 receptor (2)

A

Decrease HR
Decrease contractility of atria

Atropine inhibits M2 –> given for pts. w/ bradycardia

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109
Q

M3 receptor (6)

A

a) Increase exocrine gland secretions (lacrimal, gastric acid)
b) Increase gut peristalsis
c) Increase bladder contraction
d) Bronchoconstriction
e) Increase pupillary sphincter muscle contraction (miosis)
f) Ciliary muscular contraction (accomodation)

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110
Q

Dopamine

A

D1 - s

D2 - i

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111
Q

D1 receptor

A

Relaxes renal vascular smooth muscle (increase renal blood flow)

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112
Q

D2 receptor

A

Modulates transmitter release (esp in BRAIN)

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113
Q

Histamine

A

H1 - q

H2 - s

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114
Q

H1 receptor

A

a) Increase nasal and bronchial mucus production
b) Contraction of bronchioles
c) Pruritus
d) Pain

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115
Q

H2 receptor

A

Increase gastric acid secretion

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116
Q

Vasopressin

A

V1 - q

V2 - s

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117
Q

V1 receptor

A

Increase vascular smooth muscle contraction

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118
Q

V2 receptor

A

Increase H2O permeability & reabsorption in collecting tubules of kidney

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119
Q

Gq receptors

A

H1, a1, V1, M1, M3

“HAVe 1 M&M”

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120
Q

Function of Gq

A

Receptor –> Gq –> phospholipase C –> Lipids cleaved to PIP2; PIP2 cleaved to DAG and IP3 via phospholipase C

DAG –> protein kinase C –> phosphorylation of downstream messengers

IP3 –> Increase intracellular Ca2+ –> smooth muscle contraction

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121
Q

Qs receptors

A

b1, b2, D1, H2, V2

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122
Q

Qi receptors

A

M2, a2, D2

“MAD 2’s”

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123
Q

Function of Gs and Gi

A

Receptor –> Gs or Gi –> Adenyl cyclase –> ATP to cAMP –> protein kinase A

Protein kinase A –>

a) Increase intracellular Ca2+ (heart)
b) Myosin light chain kinase (smooth muscle)

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124
Q

Glaucoma drugs

A

Decrease intraocular pressure via decrease amount of aqueous humor (increase drainage, inhibit synthesis or secretion)

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125
Q

Types of glaucoma drugs (5)

A

1) a-agonist
2) b-blockers
3) diuretics
4) cholinomimetics
5) prostaglandin

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126
Q

Glaucoma drugs: a-agonists

A

EPI: decrease aqueous humor synthesis via VASOCONSTRICTION

Brimonidine (a2): decrease aqueous humor synthesis

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127
Q

Side effects of EPI and Brimonidine for glaucoma treatment

A

Mydriasis (dilated pupils)

Blurry vision, ocular hyperemia, foreign body sensation, ocular allergic rxns, ocular pruritus

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128
Q

What type of glaucoma should you never use EPI or Brimonidine for?

A

Closed-angle glaucoma

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129
Q

Glaucoma drugs: b-blockers

A

Timolol
Betaxolol
Carteolol

No pupillary or vision changes - no side effects!!

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130
Q

Glaucoma drugs: diuretics

A

Acetazolamide

Decrease aqueous humor synthesis via inhibition of carbonic anhydrase

No pupillary or vision changes - no side effects!!

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131
Q

Glaucoma drugs: cholinomimetics

A

Direct: pilocarpine, carbachol

Indirect: physostigmine, echotiophate

ALL increase drainage of aqueous fluid

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132
Q
Pilocarpine
Carbachol
Physostigmine
Echothiophate
(MOA)
A

Increase outflow of aqueous humor via contraction of ciliary m. –> opens trabecular meshwork

Use Pilocarpine in EMERGENCIES - very effective at opening meshwork into canal of Schlemm

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133
Q
Pilocarpine
Carbachol
Physostigmine
Echothiophate
(side effects)
A

Miosis

Cyclospasm (contraction of ciliary m.)

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134
Q

Glaucoma drugs: prostaglandin

A

Latanoprost (PGF2a)

Increase outflow of aqueous humor

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135
Q

Latanoprost (side effect)

A

Darkens color of iris (browning)

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136
Q

Opioid analgesic

A
Morphine
Fentanyl
Codeine
Heroin
Methadone
Meperidine
Dextromethorphan
Diphenoxylate
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137
Q

Opioid: MOA

A

Agonist at opioid receptors (mu = morphine, delta = enkephalin, kappa = dynorphin) –> modulates synaptic transmission

Open K+ channels –> close Ca2+ channels –> DECREASE synaptic transmission

138
Q

Opioids inhibit release of what substances?

A
ACh
NE
5-HT
Glutamate
substance P
139
Q

Opioid: Indications

A
Pain
Cough suppression
Diarrhea
Acute pulmonary edema
Maintennance programs for addicts
140
Q

What opioid is used for cough suppression?

A

Dextromethorphan

141
Q

What opioid is used for diarrhea?

A

Loperamide

Diphenoxylate

142
Q

What opioid is used for maintennace programs for addicts?

A

Methadone

143
Q

Opioid: Toxicity

A
Addiction
Respiratory depression
Constipation
Miosis (pinpoint pupils)
CNS depression (additive w/ other drugs)
144
Q

How do you treat opioid overdose?

A

Naloxone
Naltrexone

Both are opioid receptor antagonists

145
Q

Butorphanol: MOA

A

Mu opioid receptor PARTIAL agonist

Kappa opoid receptor agonist

Analgesia

146
Q

Butorphanol: Indications

A

Severe pain (migraine, labor)

Causes less respiratory depression than full opioid agonists

147
Q

Butorphanol: Toxicity

A

Opioid withdrawal symptoms if patient is also taking full opioid agonist (competition for opioid receptors)

Overdose NOT easily reversed w/ Naloxone

148
Q

Tramadol: MOA

A

Very weak opioid agonist

Inhibits serotonin and NE reuptake (works on multiple neurotransmitters)

149
Q

Tramadol: Indications

A

Chronic pain

150
Q

Tramadol: Toxicity

A

Similar to opioids

Decreases seizure threshold*

151
Q

Phenytoin: MOA

A

Blocks Na2+ channels

Inhibit glutamate release (no excitation)

152
Q

Phenytoin: Indications

A

Tonic-clonic seizures

Class IB antiarrhythmic

153
Q

Phenytoin: Toxicity (8)

A
  1. Nystagmus, diplopia, ataxia, sedation
  2. Gingival hyperplasia (children)
  3. SLE-like syndrome
  4. Induction of cytP450
  5. Megaloblastic anemia (decrease folate absorption)
  6. Tetratogenesis (fetal hydantoin syndrome)
  7. Stevens-Johnson
  8. Osteopenia
154
Q

Barbituates (4)

A

Phenobarbital
Pentobarbital
Thiopental
Secobarbital

155
Q

Barbituates: MOA

A

Increase DURATION of Cl- channels opening –> DECREASE neuron firing –> potentiates GABA action

156
Q

Barbituates: Indications

A

Sedative for:

Anxiety, Seizures, Insomnia, Induction of anesthesia

157
Q

What barbituate is used for induction of anesthesia?

A

Thiopental

158
Q

When is barbituates contraindicated?

A

Porphyria

159
Q

Barbituates: Toxicity

A

Respiratory and cardiovascular depression (can be fatal!!)

CNS depression (exacerbated w/ ethanol use)

Drug interactions (p450 inducer)

160
Q

Overdose of barbituates: treatment?

A

Supportive - assist respiration & maintain BP

161
Q

Benzodiazepines (8)

A
Diazepam
Lorazepam
Triazolam
Temazepam
Oxazepam
Midazolam
Chlordiazepoxide
Alprazolam
162
Q

Benzodiazepines: MOA

A

Increase FREQUENCY of Cl- channel opening –> potentiates GABA action

Long half lives (except Triazolam, Oxazepam, Midazolam = short acting)

163
Q

Benzodiazepines: Indications

A
Anxiety
Spasticity
Status epilepticus (lorazepam, diazepam)
Detoxification (alcohol withdrawal-DTs)
Sleep walking
General anesthetic (amnesia, muscle relaxation)
Hypnotic (insomnia)
164
Q

Which benzos are used especially for status epilepticus?

A

Lorazepam

Diazepam

165
Q

Benzodiazepines: Toxicity

A

Dependence
Additive CNS depression w/ alcohol

LESS risk of respiratory depression & coma than barbituates

166
Q

Which benzos are short acting (therefore have high addictive potential)?

A

Triazolam
Oxazepam
Midazolam

167
Q

Treatment for benzodiazepines overdose:

A

Flumazenil (competitive antagonist at GABA benzodiazepine receptor)

168
Q

Non-benzodiazepine hypnotics

A

Zolpidem (Ambien)
Zaleplon
Eszopiclone

169
Q

Zolpidem: MOA

A

Act via BZ1 subtype of GABA receptor

170
Q

Zolpidem: Indications

A

Insomnia

171
Q

Zolpidem: Toxicity

A

Ataxia, headaches, confusion

Short duration –> rapid metabolism by liver enzymes
Cause only modest day-after psychomotor depression; few amnestic effects

LOWER dependence risk than benzodiazepines

172
Q

Treatment for Zolpidem toxicity

A

Flumazenil

173
Q

Anesthetics: general principles

A

CNS drugs – must be LIPID SOLUBLE (cross BBB) or be actively transported

DECREASE solubility in BLOOD –> rapid induction/recovery

INCREASE solubility in LIPIDS –> increase potency (1/MAC) – smaller MAC equals greater potency
(MAC = minimal alveolar concentration at which 50% of pts. anesthetized)

174
Q

Halothane vs. N2O: potency and solubility profile

A

N2O has DECREASE blood and lipid solubility –> fast induction - low potency
Halothane has INCREASE blood and lipid solubility –> slow induction - high potency

175
Q

Inhaled anesthetics (6)

A

Halothane
“-flurane”: Enflurane, Isoflurane, Sevoflurane, Methoxyflurane
Nitrous oxide

176
Q

Halothane
Enflurane/Isoflurane
Nitrous oxide
(Indications)

A

MI depression
Respiratory depression

Increase cerebral blood flow (decrease cerebral metabolic demand)

177
Q

Halothane: toxicity

A

Hepatotoxic

178
Q

Methoxyflurane: toxicity

A

Nephrotoxic

179
Q

Enflurane: toxicity

A

Pro-convulsant

180
Q

All inhaled anesthetics (except nitrous oxide) have increased risk of:

A

Malignant hyperthermia

181
Q

Nitrous oxide: toxicity

A

Expansion of trapped gas in body cavity

182
Q

IV anesthetics (5)

A

Barbituates (increase duration of Cl- channels opening)
Benzodiazepines (increase frequency of Cl- channels opening)

Ketamine
Opioids
Propofol

183
Q

IV anesthetic: Thiopental

A

high potency - high lipid solubility
RAPID entry in brain
*Induction of anesthesia, short surgical procedures

effect terminated by RAPID REDISTRIBUTION into tissue (skeletal muscle) & fat

decrease cerebral blood flow (sedation/sleep effect)

Postoperative nausea

184
Q

IV anesthethic: Midazolam

A

Endoscopy

Used w/ gaseous anesthetics & narcotics

185
Q

Midazolam: toxicity

A

Severe postoperative respiratory depression
Decrease BP (treat w/ flumazenil)
Amnesia

186
Q

IV anesthetic: Ketamine

A

PCP analogs

Block NMDA receptors

Cardiovascular stimulant

187
Q

Ketamine: toxicity

A

Hallucination, bad dreams

Increase cerebral blood flow

188
Q

IV anesthetic: Opioids

A

Morphine
Fentanyl

Used w/ other drugs during general anesthesia

189
Q

IV anesthetic: Propofol

A

Sedation in ICU
Rapid anesthesia induction in short procedures

Less postoperative nausea than thiopental
Potentiates GABA

190
Q

Local anesthetics

A

Esters: Procaine, Cocaine, Tetracaine

Amides: Lidocaine, Mepivacaine, Bupivacaine

(AmIdes have 2 “I”s)

191
Q

Local anesthetics: MOA

A

Block activated Na+ channels (effective in rapidly firing neurons)

Given w/ vasoconstrictors (EPI) to enhance local action

Decrease bleeding

Increase anesthesia by decrease systemic concentration

192
Q

Local anesthetics: Indications

A

Minor surgical procedures
Spinal anesthesia

Give amides if pt. is allergic to esters

193
Q

Alkaline anesthetics in infected (acidic) tissue

A

Alkaline anesthetics are charged - can’t penetrate membrane –> need more anesthetics

194
Q

Order of nerve blockade

A

Small diameter fibers before large fibers
Myelinated fibers before unmyelinated
(SIZE matters the most!!)

195
Q

Order of sensation loss

A
  1. Pain
  2. Temperature
  3. Touch
  4. Pressure
196
Q

Local anesthetics: Toxicity

A
CNS excitation
Cardiovascular toxicity (Bupivacaine)
HTN
Hypotension
Arrhythmias (Cocaine)
197
Q

Local anesthetics: cardiovascular toxicity

A

Bupivacaine

198
Q

Local anesthetics: arrhythmias

A

Cocaine

199
Q

Neuromuscular blocking drugs: general uses

A

Muscle paralysis (relaxer) in surgery

Mechanical ventilation

Selective for motor nicotinic receptor

200
Q

Neuromuscular blocking: depolarizing

A

Succinylcholine

Strong Ach receptor agonist – SUSTAINED depolarization –> no repolarization –> no muscle contraction

201
Q

Reversal of Succinylcholine blockade

A

Phase I: prolonged depolarization - no antidote (block potentiated by cholinesterase inhibitors)

Phase II: repolarized but blocked; Ach receptors available but desensitized
Antidote for phase II: cholinesterase inhibitor (Neostigmine) –> increase Ach available so that when receptors become available –> mm. contraction resumes

202
Q

Complications of Succinylcholine

A

Hypercalcemia
Hyperkalemia
Malignant hyperthermia

203
Q

Neuromuscular blocking: nondepolarizing

A
Tubocurarine
Atracurium
Mivacurium
Pancuronium
Vecuronium
Rocuronium

Competitive antagonist - compete w/ Ach for receptors

204
Q

Reversal of Tubocurarine, Atracurium, Vecuronium

A

Neostigmine (wake patients up from surgery)
Edrophonium
& other cholinesterase inhibitors

205
Q

Dantrolene: MOA

A

Prevent release of Ca2+ from SR in skeletal muscle

206
Q

Dantrolene: Indications

A

1) Malignant hyperthermia
2) Neuroleptic malignant syndrome (toxicity of antipsychotic drugs)

Causes of malignant hyperthermia:

a) Toxicity of inhalation anesthetics (Halothane, “-flurane”); N2O does not have this side effect
b) Succinylcholine

207
Q

Parkinsonism drugs: strategy

A

Parkinsonism: decrease dopamine; excess cholinergic activity

Drug actions:

1) dopamine agonists
2) increase dopamine release
3) prevent dopamine breakdown
4) curb excess cholinergic activity

208
Q

Bromocriptine (ergot)
Pramipexole
Ropinirole (non-ergot) – preferred

A

Dopamine agonists

209
Q

Amantadine (neuro & micro indications)

A

Increase dopamine release

ANTIVIRAL against influenza A & Rubella

210
Q

Amantadine: toxicity

A

Ataxia

211
Q

L-dopa/Carbidopa

A

Converted to dopamine in CNS

L-dopa crosses BBB –> converted to dopamine in CNS via dopa decarboxylase

212
Q

Why is carbidopa given w/ L-dopa?

A

Limit peripheral side effects by inhibiting L-dopa conversion to dopamine peripherally –> increase amount of L-dopa available in the brain

213
Q

Toxicity of L-dopa/Carbidopa

A

Arrhythmias from increased peripheral formation of catecholamines

long term use: dyskinesia following administration

214
Q

Selegiline: MOA

A

Selective MAO-B inhibitor

MAO-B preferentially metabolizes dopamine over NE and 5-HT

215
Q

Selegiline: Indications

A

Adjunctive agent to L-dopa in treatment of Parkinson’s disease

216
Q

Selegiline: Toxicity

A

Enhance adverse effects of L-dopa

217
Q

Entacapone, Tolcapone

A

COMT inhibitors

Inhibit L-dopa degradation –> increase dopamine availability

218
Q

Benztropine

A

Antimuscarinic – improves tremor & rigidity (little effect on bradykinesia)

219
Q

Memantine: MOA

A

NMDAR antagonist

Prevents excitotoxicity (mediated by Ca2+)

220
Q

Memantine: Indications

A

Alzheimer’s

221
Q

Memantine: Toxicity

A

Hallucinations

Confusion

222
Q

Donepezil
Galantamine
Rivastigmine
(MOA)

A

Acetylcholinesterase inhibitors

223
Q

Donepezil
Galantamine
Rivastigmine
(Indications)

A

Alzheimer’s

224
Q

Donepezil
Galantamine
Rivastigmine
(Toxicity)

A

Insomnia

225
Q

Neurotransmitter changes in Huntington’s disease

A

Decrease GABA
Decrease ACh
Increase Dopamine

226
Q

Tetrabenazine
Reserpine
(MOA)

A

Inhibit VMAT –> limit dopamine vescile packaging & release

Rx for Huntington’s (too much dopamine)

227
Q

Haloperidol

A

Dopamine receptor antagonist

Rx for Huntington’s (too much dopamine)

228
Q

Sumatriptan: MOA

A

5-HT agonist

Inhibits trigeminal nerve

Prevents vasoactive peptide release

Induces vasoconstriction

Half life < 2hrs

229
Q

Sumatriptan: Indications

A

Acute migraine

Cluster headache attacks

230
Q

Sumatriptan: Toxicity

A

Coronary vasospasm

Mild tingling

231
Q

When is sumatriptan contraindicated?

A

Patients w/ CAD or Prinzmetal’s angina (due to coronary vasospasm side effect)

232
Q

Rx: alcohol withdrawal

A

Benzodiazepines

233
Q

Rx: anxiety

A

SSRIs
SNRIs
Buspirone

234
Q

Rx: ADHD

A

Methylphenidate

Amphetamines

235
Q

Rx: Bipolar disorder

A

Mood stabilizers:
Lithium
Valproic acid
Carbamazepine

Aytpical antipsychotics

236
Q

Rx: Bulimia

A

SSRIs

237
Q

Rx: Depression

A

SSRIs
SNRIs
TCAs
Buspirone

Mirtazapine (depression w/ insomnia)

238
Q

Rx: OCD

A

SSRIs

Clomipramine

239
Q

Rx: Panic disorder

A

SSRIs
Venlafaxine
Benzodiazepines

240
Q

Rx: PTSD

A

SSRIs

241
Q

Rx: Schizophrenia

A

Antipsychotics

242
Q

Rx: Social phobias

A

SSRIs

243
Q

Rx: Tourette’s syndrome

A

Antipsychotics (Haloperidol, Risperidone)

244
Q

CNS stimulants (3)

A

Methylphenidate
Dextroamphetamine
Methamphetamine

245
Q

CNS stimulants: MOA

A

Increase catecholamines at synaptic cleft – DOPAMINE & NE

246
Q

CNS stimulants: Indications

A

ADHD
Narcolepsy
Appetite control

247
Q

Typical Antipsychotics: “neuroleptics” (5)

A

Haloperidol

"-azines":
Trifluoperazine
Fluphenazine
Thioridazine
Chlorpromazine
248
Q

Antipsychotics (typical): MOA

A

Block dopamine D2 receptors –> increase cAMP

249
Q

Antipsychotics (typical): Indications

A

a) Schizophrenia (positive symptoms)
b) Psychosis
c) Acute mania
d) Tourette’s syndrome

250
Q

Antipsychotics (typical): Toxicity

A

Highly soluble - stored in fat - very slow removal from body

Extrapyramidal symptoms (dyskinesia)

Endocrine: dopamine receptor antagonism –> hyperprolactinemia –> galactorrhea

Blocking muscarinic: dry mouth, constipation

Block a1 receptors: hypotension

Block histamine receptors: sedation

251
Q

High potency antipsychotics

A

Trifluoperazine
Fluphenazine
Haloperidol

Extrapyramidal symptoms

252
Q

Low potency antipsychotics

A

Chlorpromazine
Thioridazine

Non-neurologic side effects (anticholinergic, antihistamine, a1-blockade)

253
Q

Chlorpromazine toxicity

A

Corneal deposits

254
Q

Thioridazine toxicity

A

reTinal deposits

255
Q

Haloperidol toxicity

A

Neuroleptic malignant syndrome

Tardive dyskinesia (involuntary repetitive motions – oral/facial motions) – usually irreversible

256
Q

Neuroleptic malignant syndrome (NMS)

A

Rigidity
Myoglobinuria
Autonomic instability
Hyperpyrexia

257
Q

Treatment for neuroleptic malignant syndrome

A

Dantrolene

D2 agonists - Bromocriptine

258
Q

Atypical antipsychotics (6)

A
Olanzapine
Clozapine
Quetiapine
Risperidone
Aripiprazole
Ziprasidone
259
Q

Atypical antipsychotics: Indications

A

a) Schizophrenia (positive & negative symptoms)
b) Bipolar disorder
c) OCD
d) anxiety
e) depression
f) mania
g) Tourette’s syndrome

260
Q

Atypical antipsychotics: Toxicity

esp. Olanzapine/clozapine; clozapine; Ziprasidone

A

LESS extrapyramidal and anticholinergic side effects than traditional antipsychotics

Olanzapine/Clozapine: weight gain

Clozapine: agranulocytosis (need WBC monitoring)

Seizure

Ziprasidone: prolonged QT interval

261
Q

Lithium: Indications

A

Mood stabilizer: bipolar disorder

Blocks relapse and acute manic events

SIADH

262
Q

What renal disorder is lithium used for?

A

SIADH

263
Q

Lithium: Toxicity

A
Tremor
Sedation
Edema
Heart block*
Hypothyroidism

Polyuria (ADH antagonist –> nephrogenic DI)

Teratogenesis (fetal cardiac defects = EBSTEIN’s anomaly; malformation of great vessels)

264
Q

Therapeutic index of Lithium

A

Narrow - requires constant monitoring of serum levels

265
Q

Lithium excretion

A

Kidneys; most reabsorbed at PCT following Na+ reabsorption

266
Q

Buspirone: MOA

A

Stimulates 5-HT receptors

267
Q

Buspirone: Indications

A

Generalized anxiety disorder

Takes 1-2 weeks to take effect

No sedation/addiction/tolerance

DOES NOT interact w/ alcohol (vs. barbituates, benzodiazepines)

268
Q

Antidepressants (4)

A

1) SSRIs
2) SNRIs
3) TCAs
4) MAO inhibitors

269
Q

SSRIs (4)

A

Fluoxetine
Paroxetine
Sertraline
Citalopram

270
Q

SSRIs: MOA

A

Serotonin-specifc reuptake inhibitors

271
Q

SSRIs: Indications

A
Depression
Generalized anxiety disorder
Panic disorder
OCD
Bulimia
Social phobias
PTSD
272
Q

SSRIs: Toxicity

A

FEWER toxicities than TCAs

GI distress

Sexual dysfunction (anorgasmia and decreased libido)

Serotonin syndrome: (also seen w/ MAO inhibitors, SNRIs, TCAs – all drugs that increase serotonin levels)

1) hyperthermia
2) myoclonus
3) cardiovascular collapse
4) flushing
5) diarrhea
6) seizures/confusion

273
Q

Treatment of serotonin syndrome

A

Cyproheptadine (5-HT2 receptor antagonist) –> DECREASE serotonin levels

274
Q

SNRIs (2)

A

Venlafaxine

Duloxetine

275
Q

SNRIs: MOA

A

Inhibit serotonin and NE reuptake

276
Q

SNRIs: Indications

A

DEPRESSION

Venlafaxine: generalized anxiety & panic disorders

Duloxetine: diabetic peripheral neuropathy (greater effect on NE)

277
Q

SNRIs: Toxicity

A

Increase BP

278
Q

TCAs

A

“-iptyline” – Amitriptyline

“-ipramine” – Imipramine, Desipramine, Clomipramine

Doxepin
Amoxapine

279
Q

TCAs: MOA

A

Blocks reuptake of NE and serotonin

280
Q

TCAs: Indications (4)

A

Major depression

Bedwetting (Imipramine)

OCD (Clomipramine)

Fibromyalgia

281
Q

TCAs: Toxicity

A

a) Sedation
b) a1 blockade –> postural hypotension
c) atropine-like side effects (anticholinergic) – tachycardia, urinary retention, dry mouth

Convulsions
Coma
Cardiotoxicity (arrhythmias)
Respiratory depression
Hyperpyrexia
282
Q

Amitriptyline vs. Nortriptyline

A

Amitriptyline has MORE anticholinergic effects than Nortriptyline

Use nortriptyline in elderly to decrease anticholinergic side effects (confusion/hallucinations)

283
Q

Which TCA has least sedating effects and lower seizure threshold (easier for seizures to occur)?

A

Desipramine

284
Q

What is given to treat arrhythmias caused by TCAs?

A

NaHCO3

285
Q

Monoamine oxidase (MAO) inhibitors

A

Tranylcypromine
Phenelzine
Isocarboxazid
Selegiline (selective MAO inhibitor)

286
Q

MAO inhibitor: MOA

A

Nonselective MAO inhibition –> increase levels of amine neurotransmitters (NE, serotonin, dopamine)

287
Q

MAO inhibitor: Indications

A

Atypical depression
Anxiety
Hypochondriasis (fear of having a malignant disease)

288
Q

MAO inhibitor: Toxicity

A

Hypertensive crises (due to ingestion of tyramine via wine&cheese)

289
Q

When is MAO inhibitor contraindicated?

A
Do not use MAO inhibitors w/:
SSRIs
TCAs
St. John's Wort
Meperidine
Dextromethorphan (to prevent serotonin syndrome)
290
Q

Atypical antidepressants (4)

A

Bupropion
Mirtazapine
Maprotiline
Trazodone

291
Q

Bupropion

A

Smoking cessation

Increase NE and dopamine

292
Q

Bupropion: toxicity

A

Tachycardia, insomnia (stimulant effects)

Seizure in bulimic patients

NO SEXUAL SIDE EFFECTS

293
Q

Mirtazapine

A

a2-antagonist –> increase release of NE and serotonin

Potent 5-HT2 and 5-HT3 receptor antagonist

294
Q

Mirtazapine: toxicity

A

Sedation (desirable in depressed pts. w/ insomnia)

Increased appetite, weight gain (desirable for elderly or anorexic pts.)

295
Q

Maprotiline

A

Blocks NE reuptake

296
Q

Maprotiline: toxicity

A

Sedation

Orthostatic hypotension

297
Q

Trazodone

A

Inhibits serotonin reuptake

Rx for insomnia – higher doses for antidepressant effects

298
Q

Trazodone: toxicity

A

Priapism (sustained erection; penis can’t relax)

Postural hypotension

299
Q

Drug rxn: coronary vasospasm

A

Cocaine
Sumatriptan
Ergot alkaloids

300
Q

Drug rxn: cutaneous flushing

A

Vancomycin
Adenosine
Niacin
Ca2+ channel blockers

301
Q

Drug rxn: dilated cardiomyopathy

A

Doxorubicin (Adriamycin)

Daunorubicin

302
Q

Drug rxn: Torsades de pointes

A
antiarrhythmics:
Class III (Sotalol)
Class IA (Quinidine)
303
Q

Drug rxn: agranulocytosis

A
Clozapine
Carbamazepine
Colchicine
Propylthiouracil
Methimazole
Dapsone
304
Q

Drug rxn: aplastic anemia

A
Chloramphenicol
Benzene
NSAIDs
Propylthiouracil
Methimazole
305
Q

Drug rxn: Direct Coombs-positive hemolytic anemia

A

Methyldopa

Penicillin

306
Q

Drug rxn: gray baby syndrome

A

Chloramphenicol

307
Q

Drug rxn: hemolysis in G6PD-deficient patients (6)

A
Isoniazid (INH)
Sulfonamides
Primaquine
Aspirin
Ibuprofen
Nitrofurantoin
308
Q

Drug rxn: megaloblastic anemia

A

Phenytoin
Methotrexate
Sulfa drugs

309
Q

Drug rxn: thrombotic complications

A

OCPs (estrogens)

310
Q

Drug rxn: cough

A

ACE inhibitors

Use ARBs - no cough

311
Q

Drug rxn: pulmonary fibrosis

A

Bleomycin
Amiodarone
Busulfan

312
Q

Drug rxn: acute cholestatic hepatitis, jaundice

A

Erythromycin

313
Q

Drug rxn: focal to massive hepatic necrosis

A

Halothane
Amanita phalloides (death cap mushroom)
Valproic acid
Acetaminophen

314
Q

Drug rxn: hepatitis

A

INH

315
Q

Drug rxn: pseudomembranous colitis

A

Clindamycin

Ampicillin

316
Q

Drug rxn: adrenocortical insufficiency

A

Glucocorticoid withdrawal (HPA suppression)

317
Q

Drug rxn: gynecomastia

A
Spironolactone
Digitalis
Ciimetidine
chronic Alcohol use
estrogens
Ketoconazole
318
Q

Drug rxn: hot flashes (2)

A

Tamoxifen

Clomiphene

319
Q

Drug rxn: hyperglycemia (5)

A
Niacin
Protease inhibitors
HCTZ
Corticosteroids
Tacrolimus (immunosupressant for transplants; eczema-atopic dermatitis)
320
Q

Drug rxn: hypothyroidism (3)

A

Lithium
Amiodarone
Sulfonamides

321
Q

Drug rxn: fat redistribution (2)

A

Glucocorticoids

Protease inhibitors

322
Q

Drug rxn: gingival hyperplasia (2)

A

Phenytoin

Verapamil

323
Q

Drug rxn: gout (4)

A

Furosemide
Thiazides
Niacin
Cyclosporine (immunosuppressant)

324
Q

Drug rxn: myopathies

A
Fibrates
Niacin
Colchicine
Hydroxychloroquine
Interferon-alpha
Penicillamine
Statins
Glucocorticoids
325
Q

Drug rxn: osteoporosis

A

Corticosteroids

Heparin

326
Q

Drug rxn: photosensitivity

A

Sulfonamides
Amiodarone
Tetracycline

327
Q

Drug rxn: rash (Stevens-Johnson syndrome)

A
Penicillin
Ethosuximide
Carbamazepine
Sulfa drugs
Lamotrigine
Allopurinol
Phenytoin
Phenobarbital
328
Q

Drug rxn: SLE-like syndrome

A

Hydralazine
Procainamide
Phenytoin
INH

SLE-like syndrome:
Joint pain & muscle pain
Inflammation of heart & lungs (pericarditis & pleuritis)
Anti-histone antibodies

329
Q

Drug rxn: teeth (kids)

A

Tetracyclines

330
Q

Drug rxn: tendonitis, tendon rupture, cartilage damage

A

Fluoroquinolones

331
Q

Drug rxn: diabetes insipidus

A

Lithium

Demeclocycline

332
Q

Drug rxn: Fanconi’s syndrome

A

Expired tetracycline

Fanconi’s syndrome: glucose, aa, uric acid, phosphate, bicarbonate passed in urine (instead of being reabsorbed)

333
Q

Drug rxn: hemorrhagic cystitis

A

Cyclophosphamide
Ifosfamide - treats testicular cancer

Prevent by administering w/ mesna

334
Q

Drug rxn: interstitial nephritis

A

Methicillin
NSAIDs
Furosemide

335
Q

Drug rxn: SIADH

A

Carbamazepine

Cyclophosphamide

336
Q

Drug rxn: Cinchonism

A

Quinidine

Quinine

337
Q

Drug rxn: Parkinson-like syndrome

A

Antipsychotics
Reserpine
Metoclopramide

338
Q

Drug rxn: Seizures

A
Isoniazid
Bupropion
Imipenem/cilistatin
Tramadol
Enflurane
Metoclopramide
339
Q

Drug rxn: Tardive dyskinesia

A

Antipsychotics

340
Q

Drug rxn: antimuscarinic

A

Atropine
TCAs
H1 blockers
neuroleptics

341
Q

Drug rxn: disulfiram-like reaction

A

Metronidazole
certain Cephalosporins
Procarbazine
1st gen sulfonylureas

342
Q

Drug rxn: nephrotoxicity/ototoxicity

A

Aminoglycosides
Vancomycin
Loop diuretics
Cisplatin