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Pharmacology Flashcards

1
Q

alpha-agonists for Tx of Glaucoma?

MOA?

A

Epi (alpha1)- decr aqueous humor synthesis via vasoconstriction
Brimonidine (alpha2)- decr aqueous humor synthesis

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2
Q

Epi and Brimonidine: adverse effects on eye?

A

Mydriasis (epi)- do NOT use in closed-angle glaucoma,

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

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3
Q

BBs for Tx of Glaucoma?

MOA?

A

Timolol, Betaxolol, Carteolol

decr aqueous humor synthesis
no pupillary or vision changes

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4
Q

Diuretic for Tx of Glaucoma?

MOA?

A

Acetazolamide

decr aqueous humor synthesis via inhibition of carbonic anhydrase
no pupillary or vision changes

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5
Q

Direct Cholinomimetics for Tx of Glaucoma?

MOA?

Adverse effects to eye?

A

Pilocarpine, Carbachol
incr outflow of aqueous humor via contraction of ciliary m. and opening of trabecular meshwork
Use Pilocarpine in emergencies- very effective at opening meshwork into canal of schlemm

Miosis, Cyclospasm

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6
Q

Indirect Cholinomimetics for Tx of Glaucoma?

MOA?

Adverse effects to eye?

A

Physostigmine, Echothiophate

incr outflow of aqueous humor via contraction of ciliary m. and opening of trabecular meshwork

Miosis, Cyclospasm

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7
Q

Prostaglandins for Tx of Glaucoma?

MOA?

Adverse effects to eye?

A

Bimatoprost, Iatanoprost (PGF2alpha)

incr outflow of aqueous humor

Darkens color of Iris (browning), eyelash growth

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8
Q

Opioid Analgesics?

A

Morphine, Fentanyl, Codeine, Loperamide, Meperidine, Dextromethorphan, Diphenoxylate, Pentazocine

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9
Q

Opioid Analgesics: MOA?

A

agonists at opioid receptors to modulate synaptic transmission- open K+ channels, close Ca++ channels–> decr synaptic transm.
Inhibit release of ACh, NE, 5-HT, glutamate, substance P

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10
Q

Opioid Analgesics: clinical use?

A 
Pain, acute pulm edema, maintenance programs for heroin addicts (methadone, Buprenrphine + Naloxone),
diarrhea (Loperamide, Diphenoxylate),
cough suppression (Dextromethorphan)
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11
Q

Opioid Analgesics: ADR?

A

Addiction, resp depression, constipation, miosis (except Meperidine –> Mydriasis), additive CNS depression w other drugs
Tolerance does not develop to miosis or constipation

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12
Q

Opioid Analgesics toxicity Tx?

A

Naloxone or Naltrexone (opioid receptor antagonist)

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13
Q

Opioid receptors?

A

mu= beta-endorphin,
delta= enkephalin,
k= dynorphin
(FA pg 499)

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14
Q

k-opioid receptor agonist and mu-opioid receptor antagonist that is used for moderate-severe pain?
ADR?

A

Pentazocine

can cause opioid withdrawal Sx if pt is also taking full opioid antagonist

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15
Q

k-opioid receptor agonist and mu-opioid receptor partial agonist that produces analgesia and is used for severe pain (ie Migraine, Labor)?

A

Butorphanol

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16
Q

Butorphanol adverse effects?

A

can cause opioid withdrawal Sx if pt is also taking full opioid agonist, and OD is NOT easily reversed by Naloxone

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17
Q

Tramadol MOA?

A

Very weak opioid agonist, also inhibits 5-HT and NE reuptake

(works on multiple neurotransmitters- “Tram it all” with Tramadol)

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18
Q

Tramadol clinical use?

ADRs?

A

Chronic pain

similar to opioids; decr seizure threshold; Serotonin syndrome

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19
Q

Barbiturates?

A

Phenobarbital, Pentobarbital, Thiopental, Secobarbital

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20
Q

Barbiturates: MOA?

A

Facilitate GABA(A) action by incr duration of Cl- channel opening, thus decr neuron firing

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21
Q

Barbiturates: CI?

A

Porphyria

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22
Q

Barbiturates: clinical use?

A

sedative for anxiety, seizures, insomnia, induction of anesthesia (thiopental)

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23
Q

Barbiturates: ADRs?

A

Resp and CV depression (can be fatal), CNS depression (worse w alcohol), dependence, drug intxns (induces cytP-450)

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24
Q

Barbiturates: OD Tx?

A

Supportive (assist resp and maintain BP)

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25
Benzos?
Diaze-, Loraze-, Temaze-, Oxaze- pam Triazolam, Midazolam, Alprazolam Chlordiazepoxide
26
Benzo MOA?
Facilitate GABA(A) action by INCR FREQUENCY of Cl- channel opening. Decr REM sleep
27
Most Benzos have long half-lives and active metabolites.. what are the exceptions?
Alprazolam, Triazolam, Oxazepam, Midazolam ("ATOM") | these are short-acting --> higher addictive potential
28
Benzos: clinical use?
Anxiety, spasticity, eclampsia, detox (esp alcohol withdrawal- DTs), night terrors, sleepwalking, Insomnia (hypnotic), Gen anesthetic (amnesia, m. relaxation), status epilepticus (lorazepam, Diazepam)
29
Benzos: ADRs?
Dependence, additive CNS depression w. alcohol. OD Tx: Flumazenil, can ---> seizures bu causing acute benzo withdrawal LESS risk of resp depression/coma than w Barbs
30
What are the Nonbenzodiazepine Hypnotics?
Zolpidem, Zaleplon, esZopiclone | "All ZZZs put you to sleep"
31
Nonbenzodiazepine Hypnotics: MOA?
act via the BZI subtype of the GABA receptor Sleep cycle less affected compared to benzos and less risk of dependence Effects reversed by Flumazenil
32
Nonbenzodiazepine Hypnotics: clinical use? ADRs?
Insomnia Ataxia, HAs, confusion. Rapidly metabolized by liver enzymes --> short duration (Unlike other hypnotics, cause only modest day-after psychomotor depression and few amnestic effects)
33
MAC of inhaled anesthetics?
=Minimal Alveolar Conc. required to prevent 50% of subjects from moving in response to noxious stimulus
34
Anesthetics w incr solubility in lipids have ?
incr potency (=1/MAC) | CNS drugs must be lipid soluble to cross BBB or be actively transported
35
Anesthetics w decr solubility in blood -->
rapid induction and recovery times
36
inhaled anesthetics?
Desflurane, Halothane, Enflurane, Isoflurane, Sevoflurane, Methoxyflurane, N2O (MOA unknown)
37
inhaled anesthetics: effects?
Myocardial and resp depression, N/V, incr cerebral blood flow (decr cerebral metabolic demand)
38
inhaled anesthetics: ADRs?
``` Malignant Hyperthermia Hepatotoxicity (Halothane) Nephrotoxicity (Methoxyflurane) Proconvulsant (Enflurane) Expansion of trapped gas in a body cavity (N2O) ```
39
Malignant Hyperthermia?
Rare, life threatening, inhaled anesthetics or Succinylcholine induce fever/severe m. contractions. Susceptibility inherited AD w. variable penetrance. Mutations in voltage-gated ryanodine receptor --> incr Ca++ release for SR
40
Malignant Hyperthermia and neuroleptic malignant syndrome Tx?
Dantrolene (ryanodine receptor antagonist- prevents release of Ca++ from SR of skeletal m.)
41
IV anesthetics?
THiopental (barb), Midazolam (Benzo), Ketamine, Propofol, OPioids ("THe Mighty King Proposes foolishly to Oprah")
42
Thiopental as an IV anesthetic?
High potency, high lipid solubility, rapid entry into brain. Used for induction of anesthesia and short surgical procedures. Effect terminated by rapid redistribution into tissue/fat. decreases cerebral blood flow
43
IV anesthetic commonly used for endoscopy (used adjunctively w gaseous anesthetics and narcotics)? ADRs?
Midazolam severe post-op resp depression, decr BP (OD Tx= Flumazenil), Anterograde amnesia
44
PCP analogs that act as dissociative anesthetics, Block NMDA receptors, CV stimulants?
Arylcyclohexylamines (Ketamine)
45
Arylcyclohexylamines (Ketamine) ADRs?
Disorientation, hallucinations, bad dreams, increased cerebral blood flow
46
IV anesthetic used for sedation in ICU, rapid anesthesia induction, short procedures. Potentiates GABA(A) Less post-op nausea than Thiopental.
Propofol
47
L-dopa (Levodopa)/Carbidopa: clinical use?
Parkinson Disease
48
L-dopa (Levodopa)/Carbidopa: general MOA?
incr level of dopamine in brain | unlike dopamine, L-dopa can cross BBB and is cnvtd by dopa decarboxylase in the CNS to dopamine
49
Carbidopa: MOA
peripheral DOPA decarboxylase inhibitor | Is given w L-dopa to incr bioavailability of L-dopa in the brain and to limit peripheral side effects
50
L-dopa (Levodopa)/Carbidopa: ADRs?
Arrhythmias (from incr peripheral formation of catecholamines) Long term use: Dyskinesia then akinesia between doses ("on-off" phenomenon)
51
Selegline, Rasagiline: clinical use? ADRs?
Adjunctive agent to L-dopa in Tx of Parkinson disease may enhance ADRs of L-dopa
52
Selegline, Rasagiline: MOA?
selectively inhibit MAO-B (metabolize dopamine) --> incr dopamine availability
53
Drugs used to treat Alzheimers?
Memantine, Donepezil, galantamine, rivastigmine, tacrine
54
Donepezil, galantamine, rivastigmine, tacrine: MOA? ADRs?
AChE inhibitors (used in Tx of Alzheimers); Nausea, dizziness, insomnia
55
Memantine MOA
NMDA receptor antagonist | helps prevent excitotoxicity (mediated by Ca++)
56
Memantine ADRs?
dizziness, confusion, hallucinations
57
Huntington Disease Drugs?
Tetrabenazine and Reserpine: inhibit VMAT --> decr dopamine vesicle packaging/release (FA pg 505) Haloperidol: D2 receptor antagonist
58
Tx for ALS that modestly incr survival by decr glutamate excitotoxicity via an unclear mech?
Riluzole | "for Lou Gehring disease, give riLUzole"
59
5-HT (1B/1D) agonists. Inhibit trigeminal n. activation; prevent vasoactive peptide release; induce vasoconstriction; Used for acute migraines/ cluster HA attacks?
Sumatriptan
60
Sumatriptan: ADRs? | CIs?
Coronary vasospasm, mild paresthesia CI in pts w/ CAD or Prinzmetal angina
61
Parkinson Disease drugs?
Bromocriptine, Amantadine, Levodopa (w. carbidopa), Selegline (and COMT inhibitors), Antimuscarinics
62
Antimuscarinic used in Tx of Parkinson Disease to curb excess cholinergic activity? effects?
Benzotropine- improves tremor and rigidity but has little effect on bradykinesia ("Park your Benz")
63
Drugs used in Tx of Parkinson Disease that prevent dopamine breakdown?
Selegline (selectively inhibits MAO-B), | Tolcapone (inhibits central COMT)
64
Drug used in Tx of Parkinson Disease to increase dopamine availability by incr release and decr reuptake? Toxicity=?
Amantadine ; Ataxia, livedo reticularis
65
Drugs used in Tx of Parkinson Disease that prevent peripheral L-dopa degradation --> incr availability?
Levodopa, Tolcapone, Entacapone
66
Drug used for muscle spasms (acute low back pain) by activating GABA(B) receptors at spinal cord level --> skeletal m. relaxation?
Baclofen
67
Centrally acting skeletal m. relaxant used for muscle spasms?
Cyclobenzaprine | related to TCAs, similar anticholinergic ADRs
68
Strong ACh receptor agonist --> sustained depol. and prevents m. contraction?
Succinylcholine (Depolarizing NM blocking drug)
69
Nondepolarizing NM blocking drugs?
Tubocurarine, Atracurium, Mivacurium, Pan-, Ve-, Ro- curonium Competitive antagonists, compete w ACh for receptors
70
Local anesthetics: Esters?
Procaine, Tetracaine, Cocaine, Benzocaine
71
Local anesthetics: Amides?
Lidocaine, Mepivacaine, Bupivacaine | Amides have 2 i's in name, esters have 1
72
Local anesthetics: clinical use?
minor surgeries, spinal anesthesia | if allergic to esters give amides
73
Local anesthetics: ADRs?
CNS excitation, HTN, hypoTN, arrhythmias (cocaine), severe CV toxicity (bupivacaine)
74
Local anesthetics: order of nerve blockade
Small myelinated fibers>small unmyelinated fibers>Large myelinated fibers>Large unmyelinated fibers Order of Loss: 1) pain, (2) temp, (3) touch, (4) pressure
75
Local anesthetics: MOA?
Block Na+ channels | most effective in rapidly firing neurons
76
Primidone is metabolized to ?
phenobarb
77
Which two β-blockers are commonly prescribed for variceal bleeding?
Nadolol and propranolol
78
Increased peripheral dopamine can cause N/V. Carbidopa attenuates this effect, how?
inhibits DOPA decarboxylase, thus reduces peripheral conversion of L-DOPA into dopamine

Step 1 Neurology (3 decks)

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