Drugs to Know Exam 2 Flashcards
(122 cards)
1
Q
Mecamylamine
A
Nn antagonist
2
Q
Varenecline (Chantix)
A
- Nn partial agonist
- used to help quit smoking
- ADE: neuropsychiatric sx, sedation/insomnia, risk of cardio events, allergic rxn
3
Q
Succinylcholine
A
- Noncompetitive, depolarizing Nm blocker
- paralytic d/t too much Ach activity
- ADE: muscle fasciculations, hyperkalemia, malignant hyperthermia
4
Q
Curare derivatives (Rocuronium)
A
- Competitive Nm blocker
- paralytic
- can be outcompeted with addition of more Ach
5
Q
Nicotine
A
- Agonist at nicotinic receptors, noncompetitive
- initially turns on Nn (and Nm at high doses) but stays bound leading to depolarizing blockade and desensitization
- ADE: HA, nausea, diarrhea, nightmares, toxicity (SLUD, sweating, hypertension)
- Pts who use the patch should be warned of toxicity if they continue to smoke
6
Q
Pilocarpine
A
- Direct muscarinic agonist that enters the CNS
- Causes hypotension by activating M3 receptors on vasculature
- used in glaucoma
- rarely used systemically
7
Q
Bethanechol
A
- Direct muscarinic agonist that DOES NOT enter the CNS
- indicated for post-op and neurogenic urinary atony, also to increase peristalisis
8
Q
Methacholine
A
- Direct muscarinic agonist that DOES NOT enter the CNS
- used to diagnose reactive airway disease
9
Q
Donepezil
A
- Indirect cholinergic agonist with CNS activity
- Reversible
- used to slow progression of Alzheimer’s
10
Q
Physostigmine
A
- Indirect cholinergic agonist with CNS activity
- Irreversible
- Primarily used to counteract CNS effects of antimuscarinic drugs
11
Q
Edrophonium
A
- Indirect cholinergic agonist that works in periphery
- Reversible/short term irreversible
- used to treat/diagnose myasthenia gravis
- used to reverse the paralytic effect of Nm antagonists
- very short acting
12
Q
Neostigmine
A
- Indirect cholinergic agonist that works in periphery
- Reversible/short term irreversible
- used to treat/diagnose myasthenia gravis
- used to reverse the paralytic effect of Nm antagonists
13
Q
Pyridostigmine
A
- Indirect cholinergic agonist that works in periphery
- Reversible/short term irreversible
- used to treat/diagnose myasthenia gravis
- used to reverse the paralytic effect of Nm antagonists
14
Q
Malathion
A
- organophosphate AchE inhibitor
- causes SLUD, bradycardia, bronchospasm, bronchorrhea, muscle fasciculation, HTN
- Death by paralysis of respiratory muscles
15
Q
Sarin
A
- organophosphate AchE inhibitor
- causes SLUD, bradycardia, bronchospasm, bronchorrhea, muscle fasciculation, HTN
- Death by paralysis of respiratory muscles
16
Q
Tabun
A
- organophosphate AchE inhibitor
- causes SLUD, bradycardia, bronchospasm, bronchorrhea, muscle fasciculation, HTN
- Death by paralysis of respiratory muscles
17
Q
Pralidoxime
A
- used as treatment for organophosphate toxicity
- prevents “aging”
18
Q
Antidotes for Ach increases
A
- atropine to block M receptors
- pralidoxime to prevent aging
19
Q
Antimuscarinics (trops and scops)
- atropine, benztropine, ipratropium, tiotropium, scopolamine, tropicamide
A
- effects look much like stimulation of sympathetic
- mydriasis, cycloplegia
- does not effect vascular tone
- used in Parkinson’s and movement disorders, vertigo, motion sickness, asthma, COPD, decrease intestinal motility
20
Q
Onabotulinum toxin A (Botox)
A
- inhibits release of Ach via cleaving SNAP-25
21
Q
Contraindications of Antimuscarinics
A
- glaucoma, hypersensitivity, chronic renal and liver disease, heart disease (d/t increased HR), head irradiation
22
Q
Contraindications of Antimuscarinics
A
- glaucoma, hypersensitivity, chronic renal and liver disease, heart disease (d/t increased HR), head irradiation
- increased sensitivity in diabetics and geriatric patients
23
Q
Side effects of Antimuscarinics
A
- hot dry skin, hallucinations, delirium, urinary retention, tachycardia, palpitations, dry mouth, blurred vision
24
Q
Dobutamine
A
- direct beta agonist
- B1>B2
- ADE: tachycardia, arrhythmia, hypotension
- Cross BBB
25
Albuterol/Levalbuterol
| Salmeterol
- direct beta agonist
- B2>B1
- used to treat bronchospasm and to shift K+ intracellularly in hyperkalemia
- ADE: tachycardia, muscle tremor, nervousness, hyperglycemia
- Cross BBB
26
Phenylephrine
- direct alpha agent
- A1>A2
- mydriasis (without cycloplegia like M agonists)
- used as a topical decongestant but should not be used for more than 3 days in a row bc rebound congestion may occur
- ADE: necrosis on extravasation, bradycardia, anxiety, piloerection
27
Clonidine
- direct alpha agent
- A2>A1
- ADE: withdrawal phenomenon --> HTN, anxiety, rebound tachycardia
28
Amphetamine
- increase CNS release of NE and DA
- effects: mydriasis, tachy, euphoria, vigilance, insomnia, HTN, anxiety
- no withdrawal but very addicting
- indirect agonist
29
Cocaine
- inhibits reuptake of NE and DA
- blocks NA channels to produce local anesthesia
- effects: local numbness, tachycardia, vasoconstriction, euphoria, paranoia
- withdrawal phenomenon: intense crash
- indirect agonist
30
Phenelzine
- MAOa inhibitor to inhibit degradation of NE, DA and serotonin
- may cause **tyrosine rxn** -->tyramine causes release of NE so when tyramine is consumed and NE cannot be broken down it leads to a hypertensive crisis
- indirect agonist
31
Ephedrine and pseudoephedrine
- ephedrine restricted in US d/t increased risk of stroke
- pseudophedrine is a precursor for meth, used as a decongestant
- ADE: mydriasis, dry mouth, HTN, tachycardia, insomnia, MI
- DI: MAOI
- indirect agonist
32
Epinephrine
- B2>B1>A1
- NO risk of necrosis
- ADE: bronchodilation, HTN, arrhythmia
33
Caffeine
- inhibits PDE therefore increases cAMP
34
Caffeine
- inhibits PDE therefore increases cAMP
| - indirect agonist
35
Caffeine
- inhibits PDE therefore increases cAMP
| - indirect agonist
36
Phentolamine
- non-selective A antagonist
- use: antidote for catecholamine extravasation, to treat high blood pressure of pheochromocytoma
- effects: miosis, decreased sphincter tone, vasodilation, edema (d/t increased pressure in the capillaries)
37
Phenoxybenzamine
- non-selective A antagonist
- irreversible
- use: antidote for catecholamine extravasation, to treat high blood pressure of pheochromocytoma
- effects: miosis, decreased sphincter tone, vasodilation, edema (d/t increased pressure in the capillaries)
38
Doxazosin
- relatively selective A1 antagonist
- blocks all 3 subtypes
- used in HTN
- **ADE: first dose syncope (go low, go slow), hypotension, reflex tachycardia
39
Tamsulosin
- A1 selective antagonist
- only Aa in the urinary tract
- used in prostate hyperplasia ***
- **ADE: first dose syncope (go low, go slow), hypotension, reflex tachycardia
40
Propranolol
- Non-selective B antagonist (end in -olol, start with N-z)
- ADE: depression, erectile dysfunction
- abrupt withdrawal may cause extreme HTN and/or MI
41
B1 selective antagonists - esmolol, metoprolol
| end in -olol and start with a-m
- decrease HR, decreases contractility of heart, reduces activation of renin system
- better for lungs, hypoglycemic response, peripheral vascular disease pts
42
Carvedilol
- A1 selective, B non-selective antagonist
| - decreases BP without reflex increase in HR
43
Sotalol
- antiarrhythmic beta-blocker
44
Sotalol
- antiarrhythmic beta-blocker
45
Beta-2 blockers and hypoglycemia
- body's response to low blood sugar is to increase Epi and Ach leading to anxiety, tremor, tachycardia and sweating
- when on a beta blocker the only sign of sympathetic response will be sweating (b/c sweat glands are muscarinic)
46
Timolol
- non-specific beta antagonist
| - used in glaucoma to prevent mydriasis
47
Fenoldopam
- D1 agonist used to treat hypertensive emergency by causing vasodilation and reflex increase in HR
- used for periphery
48
Bupropion
- DA reuptake blocker (blocks DAT), indirect agonist
- atypical antidepressant
- may increase risk of seizures ** especially in women with h/o eating disorders or at high doses
49
Clozapine
- 5Ht2A/C antagonist that increases DA in the mesocortical pathway (treat negative sx)
- **may cause neutropenia, monitor WBC weekly
- may cause weight gain
- atypical antipsychotic
50
Lithium
- thought to reduce signaling of NE and DA via inhibition of inositol recycling
- controls manic phase of bipolar
- ADH: nephrogenic diabetes, hypothyroidism
- has a low therapeutic index so must be monitored
- **hyponatremia increases lithium reabsorption and increases toxicity risk
51
Dopamine agonists - Bromocriptine and Ropinirole
- ADE: hypotension, nausea, vomiting, dyskinesia, hallucinations, psychosis, impulsivity
52
Dopamine agonists - Bromocriptine and Ropinirole
- ADE: hypotension, nausea, vomiting, dyskinesia, hallucinations, psychosis, impulsivity
53
Haloperidol
- D2 antagonist used to decrease hallucinations and agitated behaviors
- minimal M1, H1 or A1 block
54
Dopamine agonists used for CNS - Bromocriptine and Ropinirole
- ADE: hypotension, nausea, vomiting, dyskinesia, hallucinations, psychosis, impulsivity
55
Metoclopramide
- blocks D2 to treat gastroparesis/reflux/nausea
56
Chlorpromazine
- low potency D2 with high M1, H1, and A1 block
- used for nausea, vomiting, cough
- high potency antipsychotic
57
Olanzapine
- 5Ht2 block
| - ADE: weight gain, diabetes, metabolic syndrome
58
Olanzapine
- 5Ht2 block
| - ADE: weight gain, diabetes, metabolic syndrome
59
Olanzapine
- 5Ht2 block
- ADE: weight gain, diabetes, metabolic syndrome
- atypical antipsychotic
60
Levodopa and carbidopa
- increase dopamine synthesis
61
Buspirone**
- 5HT1a partial agonist
- used for anxiety
- decreases NT release
- MUST BE TAKEN ROUTINELY
- ADE: nausea, sedation, dizziness
62
Sumatriptan
- 5HT1B/D agonist
- vasoconstriction in CNS vascular smooth muscle, reduce release of neuropeptides
- used to stop migraines
- ADE: chest tightness, paresthesia, flushing
- contraindicated in CAD, HTN, liver/renal disease
63
Lasmiditan
- 5HT1F agonist
- does not produce significant vasoconstriction but reduces neuroinflammation by inhibiting CGRP release
- used for migraines
64
Lorcaserin
- 5HT2C agonist
- used for weight loss
- ADE: priapism
65
Tegaserod
- 5HT4 agonist
66
LSD
- strong 5HT agonist at 5HT2A receptors
| - diminishes thalamic gating
67
Sertraline
- SSRI
68
Ergot/ergotamine
- 5HT agonist
- alpha 1 agonist: gangrene, miscarriage
- DA agonism: loss of breast milk
69
Fluoxetine (Prozac)
- SSRI
- Drug i/as: serotonin syndrome (clonus), CYP450 inhibition
- ADE: sexual dysfunction, manic activation (d/t increase in DA in limbic system), increased anxiety at start, increased risk of suicidal ideation in young people
70
Sertraline (Zoloft)
- SSRI
- Drug i/as: serotonin syndrome (clonus), CYP450 inhibition
- ADE: sexual dysfunction, manic activation (d/t increase in DA in limbic system), increased anxiety at start, increased risk of suicidal ideation in young people
71
St. John's Wort
- indirect serotonin agonist
| - **inducer of CYP3A4 and can decrease efficacy of many other drugs**
72
Trazodone
- SPARI (serotonin partial agonist reuptake inhibitor)
- increases release of NE and DA in prefrontal cortex
- ** causes priapism**
- used to treat insomnia from other antidepressants
73
Cyproheptadine
- serotonin antagonist
- used to treat serotonin syndrome
- ADE: weight gain with risk if metabolic syndrome
74
Ondansetron
- 5HT3 antagonist
| - antiemetic
75
SSRI discontinuation syndrome
- cluster of sx: dizziness, fatigue, HA, nausea, anxiety, diaphoresis, insomnia, tremor
- ** agents with longer half lives and active metabolites cause fewer/less severe sx**
76
SSRI discontinuation syndrome
- cluster of sx: dizziness, fatigue, HA, nausea, anxiety, diaphoresis, insomnia, tremor
- ** agents with longer half lives and active metabolites cause fewer/less severe sx**
77
Amitriptyline
- tricyclic antidepressant
- blocks 5HT and NE reuptake
- DI: SSRI, MAOI, CNS depressants
- actions: A1 block, antimuscarinic, H1 receptor block, Na channel block, increased serotoninergic actions
- DO NOT cause HTN (differ from SNRIs)
- TOXIC: acidosis and arrhythmia, treat with bicarb
78
Nortriptyline
- tricyclic antidepressant
- blocks 5HT and NE reuptake
- DI: SSRI, MAOI, CNS depressants
- actions: A1 block, antimuscarinic, H1 receptor block, Na channel block, increased serotoninergic actions
- DO NOT cause HTN (differ from SNRIs)
- TOXIC: acidosis and arrhythmia, treat with bicarb
79
Benzodiazepines (-zolams and -zepams)
| Alprazolam, Chlordiazepoxide, Clonazepam, Diazepam, Lorazepam, Midazolam, Oxazepam
- bind to GABAa and increase frequency of opening of the Cl channel
- low dose: anxiolytic, sedative
- high dose: hypnotic, anesthetic, muscle relaxant
- Uses: anticonvulsant **status epilepticus**
- **ADE: incoordination (DUI risk), anterograde amnesia, tolerance/dependance - abrupt withdrawal may cause seizures
- benzo withdrawal can be life threatening
80
Flumazenil
```
Benzo antagonist (antidote)
**may cause seizures in pts who are dependent on benzos**
```
81
Isoniazid
**used for TB but can deplete Vit B6 stores (pyridoxal 5' phosphate) which is needed to convert glutamate to GABA --> can cause seizures in malnourished pts
82
Benzos that are safe for pts with liver probs
Oxazepam, lorazepam, temazepam
| give these to pts with alcohol addiction
83
Barbiturates (Phenobarbital)
- bind to GABAa and keep Cl- channel open longer
- used as an anticonvulsant
- very sedating, addicting and toxic
- death d/t suppression of respiratory drive
- CYP450 enzyme inducers (like St. John's Wort)
- No muscle relaxant effects
84
The ZZZ drugs - Eszopiclone, Zaleplon, Zolpidem
- short term hypnotics
- no anticonvulsant or muscle relaxant activity
- ADE: anterograde amnesia, dependence/withdrawal, hangover, HA
85
Etomidate
- injectable anesthetic
- GABAnergic
- no change in BP
- inhibits cortisol synthesis
86
Propofol, Fospropofol
- injectable anesthetic
- anesthesia induction and maintenance
- side effect: antiemetic
- GABAnergic
87
Baclofan
- GABA-b agonist
- used for spasticity
- ADE: ataxia, sedation, blurred vision, hypotension, cardiac depression
- withdrawal: increased spasticity, pruritus, delirium, rhabdomyolosis
88
Suvorexant
- orexin A/B antagonist
- promotes sleep
- pts should not drink or drive while taking
- may cause a hangover
89
Treat ethanol withdrawal with?
- Lorazepam
- Oxazepam if no liver disease
- sx of withdrawal: tremors, hallucinations, seizures, delirium tremens, confusion, hyperthermia
90
Why is thymine replacement used in alcoholics?
To prevent Wernicke's encephalitis
91
Why is Disulfram used to help stop drinking?
It increases amount of acetaldehyde while drinking making the pt feel sick and not want to drink anymore
92
Blood:gas partition coefficient
- ratio of concentration of anesthetic in blood to gaseous state
- higher B:G = slower onset
93
MAC50
- minimal alveolar concentration needed to produce anesthesia in 50% of population
- smaller dose = more potent
94
Adverse effects of inhaled anesthesia
| NO, desflurane, sevoflurane
- **malignant hyperthermia**
| - changes in CNS flow, decreased myocardial contractility, decrease BP, irritate airways
95
Malignant hyperthermia
- hereditary mutation in ryanodine receptors leading to excess Ca++ from SR
- sx: rhabdomyolosis, hyperthermia, tachypnea, tachycardia, rigidity, acidosis
96
Treatment of malignant hyperthermia
Dantrolene
97
Dexmedetomidine
- injectable anesthetic
- Alpha 2 agonist
- may cause bradycardia and hypotension d/t decreased NE release
98
Ketamine (CIII)
- injectable anesthetic
- NMDA antagonist
- causes dissociative amnesia
- analgesia and potent bronchodilator
99
Fentanyl
- injectable anesthetic
| - Mu opiod agonist
100
Local anesthetics
- Esters: 1 i
- Amides: more than 1 i
- weak bases, mixing with bicarb will increase rate of onset and duration (and reduce pain)
- the more lipophilic the greater the potency
- amides are hepatically metabolized
- **ADE: Allergy - cross sensitivity of ester with ester and amide with amide
- ** Do not inject with a vasoconstrictor in areas with limited blood supply, but adding epi can slow systemic absorption
- repeated injections can result in tachyphylaxis
101
Carbamazepine
- inhibition of NA+ voltage gated channels
- ADE: aplastic anemia, Steven's-Johnson syndrome (screen pts of Asian ancestry), SIADH, enzyme inducer, **autoinduction**
102
Phenytoin
- inhibition of NA+ voltage gated channels
- ADE: nystagmus (at toxic levels), gingival hyperplasia, teratogenic, folate depletion, enzyme inducer
- ** saturable, zero order kinetics** --> if you double the dose you get more than double the serum concentration
103
Lamotrigine
- inhibition of NA+ voltage gated channels
| - ADE: monitor for rash
104
Topiramate
- inhibition of NA+ voltage gated channels
- does not cause weight gain
- can cause kidney stones
105
Valproate, Divalproex, Valproic acid
- Ca++ (T-type) channel blocker, also blocks Na and enhances GABA
- broadest spectrum of antiepiletics
- minimal sedation, hepatotoxic (monitor)
- inhibits metabolism of other drugs but won't reduce efficacy of contraceptives
106
Ethosuximide
- Blocks Ca++ T-type channels
- **only used for absence seizures**
- does not cause weight gain
107
Gabapentin
- Enhances GABA release
- Blocks high voltage Ca++ channels
- saturable absorption
108
Magnesium
- Blocks HVA Ca++ and NMDA gated Ca++ channels
109
Which antiepileptic drugs do not cause weight gain?
- Topiramate and ethosuximide
110
Pregabalin
- blocks HVA channels, inhibits glutamate release
111
Causes of Status Epilepticus
- nonadherence to antiepileptic meds
- withdrawal from GABAergics (and use of Flumazenil)
- Bupropion
- Isoniazid (d/t B6 depletion)
112
Treatment of Status Epilepticus
- Benzo first to break the seizure followed by phenytoin to prevent recurrence
113
Opioid full agonists - Fentanyl, Hydrocodone, Hydromorphone, Meperidine, Methadone, Morphine, Oxycodone
- C's converted to more potent M's by CYP2D6
| - methadone: very long half life, less euphoria, blocks NMDA also and inhibits serotonin reuptake
114
Opioid partial agonists - Buprenorphine, Butorphanol, Nalbuphine
- moderate pain relief but can out-compete full agonists
115
Tramadol
- Opiate SNRI
116
Tramadol
- Opiate SNRI
- weak mu agonist but mostly blocks reuptake of serotonin and NE
- can cause seizures
117
Naloxone (Narcan)
- Competitive opioid antagonist
118
Opioid withdrawal
- increased pain, dysphoria, diarrhea, yawning, mydriasis, piloerection and sweating
119
Opioid withdrawal
- increased pain, dysphoria, diarrhea, yawning, mydriasis, piloerection and sweating
120
- Carisoprodol
- GABAergic muscle relaxant
121
Cyclobenzaprine
- muscle relaxant
| - blocks reuptake of 5HT and NE, blocks A1, antimuscarinic
122
Tizanidine
- muscle relaxant
- short-acting alpha-2 agonist
- ADE: hypotension and bradycardia (decreased NE release)
