Neurology: Pharmacology

Front 1

name Parkinson's drugs

Back 1

BROMOCRIPTINE, AMANTADINE, LEVODOPA (w/carbidopa), SELEGILINE (and COMT inhibitors), antimuscarinics (eg BENZOTROPINE)

Front 2

what parkinson drugs act to increase DA levels?

Back 2

L-dopa/carbidopa, amantidine

Front 3

why is L-dopa paired with carbidopa?

Back 3

tho L-dopa crosses BBB, a large % will be decarboxylated to DA in periph, so it is paired w/carbidopa, a DA decarboxylase inhib that does not cross the BBB

Front 4

toxicity of L-dopa?

Back 4

arrhythmias from periph conversion to DA; long term use can cause dyskinesia after admin, and akinesia b/t doses (="on-off phenomenon")

Front 5

what parkinson drugs act to agonize DA receptors?

Back 5

BROMOCRIPTINE, PRAMIPEXOLE, ROPINIROLE

Front 6

MoA of BROMOCRIPTINE?

Back 6

D2 agonist and D1 antagonist

Front 7

Clinical uses of BROMOCRIPTINE?

Back 7

parkinson's, **hyperprolactinemia**, suppression of lactation in non-nursing moms, acromegaly (mediated by D1 antag, b/c DA increases GH s/c)

Front 8

what class is BROMOCRIPTINE in?

Back 8

ergot alkaloid

Front 9

what parkinson drugs act to prevent DA breakdown?

Back 9

SELEGILINE (MAO-B inhib); ENTACAPONE, TOLCAPONE (COMT inhibitors)

Front 10

what drug is SELEGILINE usu paired with?

Back 10

is used as adjunctive agent w/ L-dopa, but may also enhance adverse effects of L-dopa

Front 11

what parkinson drugs act to curb excess cholinergic activity?

Back 11

antimuscarinics, eg BENZTROPINE

Front 12

BENZTROPINE has the greatest effect on which parkinson's sx?

Back 12

tremor, rigidity; but little effect on bradykinesia

Front 13

MoA of SUMATRIPTAN?

Back 13

5HT1D agonist, causes vasoconstriction

Front 14

clinical uses of SUMATRIPTAN?

Back 14

acute migraine, cluster headache attacks

Front 15

toxicity of SUMATRIPTAN? contraindications?

Back 15

coronary vasospasm, mild tingling; contraind in pts with CAD or prinzmetal's angina

Front 16

toxicity of BENZODIAZEPINES?

Back 16

sedation, tolerance, dependence, additive CNS depress w/etoh (less risk of cardioresp dep/coma than barbs)

Front 17

toxicity of CARBAMAZEPINE?

Back 17

diplopia, ataxia, blood dyscrasias (agranulocytosis, aplastic anemia), liver tox, teratogenesis, induction of P450

Front 18

toxicity of ETHOSUXIMIDE?

Back 18

GI distress, lethargy, headache, urticaria, Stevens-Johnson syndrome

Front 19

toxicity of PHENOBARBITAL?

Back 19

sedation, tolerance, dependence, induction of P450 (thus many drug interactions), cardioresp depress (->death), additive CNS depress w/etoh

Front 20

toxicity of PHENYTOIN?

Back 20

nystagmus, diplopia, ataxia, sedation, SLE-like syndrome, induction of P450; w/chronic use: gingival hyperplasia in kids, periph neuropathy, hirsutism, megaloblastic anemia (dec folate absor), malig hypertherm (rare); teratogenic (fetal hydantoin synd)

Front 21

toxicity of VALPROIC ACID?

Back 21

GI distress, rare but fatal hepatotoxicity (measure LFTs), neural tube defects in fetus (spina bifida), tremor, weight gain

Front 22

toxicity of LAMOTRIGINE?

Back 22

Steven-Johnson synd

Front 23

toxicity of GABAPENTIN?

Back 23

sedation, ataxia

Front 24

toxicity of TOPIRAMATE?

Back 24

sedation, mental dulling, kidney stones, weight loss

Front 25

MoA of PHENYTOIN?

Back 25

use dependent blockade of Na channels (binds when in inactivated state and prolongs refrac period), inhib' glutamate release from excitatory presyn neurons

Front 26

clinical uses of PHENYTOIN?

Back 26

first line tonic clonic, first line status epilepticus prophylaxis, also used for partial seizures; also used as class IB antiarrhythmic

Front 27

MoA of CARBAMAZEPINE?

Back 27

use dependent blockade of Na channels (binds when in inactivated state and prolongs refrac period)

Front 28

clinical uses of CARBAMAZEPINE?

Back 28

1st line tonic clonic
1st line trigeminal neuralgia
good for partial seiz
2nd line bipolar d/o

Front 29

MoA of LAMOTRIGINE?

Back 29

blocks voltage-gated Na channels

Front 30

clinical uses of LAMOTRIGINE?

Back 30

partial, tonic clonic

Front 31

MoA of GABAPENTIN?

Back 31

increases GABA release

Front 32

clinical uses of GABAPENTIN?

Back 32

partial, tonic clonic, peripheral neuropathies (neuropathic pain syndromes)

Front 33

MoA of TOPIRAMATE?

Back 33

inactivates Na channels (same as phenytoin, carbamazapine); potentiates GABA-ergic transmiss; blocks glutamate at AMPA/kainate receptors

Front 34

clinical uses of TOPIRAMATE?

Back 34

partial, tonic clonic

Front 35

MoA of PHENOBARBITAL?

Back 35

inc GABA-A action by inc DURATION of Cl channel opening, thus dec neuronal firing

Front 36

can barbituates alone be lethal?

Back 36

yes; b/c at high doses, barbs can directly activate GABA channel

Front 37

clinical uses of PHENOBARBITAL?

Back 37

partial, tonic clonic
1st line in pregnant women, kids

Front 38

contraindic of BARBITUATES?

Back 38

**porphyria**

Front 39

tx of BARBITUATE o.d.?

Back 39

sx management (assist respirations, inc BP, etc)

Front 40

MoA of VALPROIC ACID?

Back 40

inc GABA accumulation, inc Na channel inactivation

Front 41

clinical uses of VALPROIC ACID?

Back 41

1st line myoclonic, tonic clonic
partial
absence (2nd line unless pt has other seizures too)
mood stabilizer in mania

Front 42

MoA of ETHOSUXIMIDE?

Back 42

blocks low-threshold T-type Ca channels (provide pacemaker current in thalamic neurons)

Front 43

clinical uses of ETHOSUXIMIDE?

Back 43

1st line absence seizures

Front 44

MoA of BENZODIAZEPINES?

Back 44

enhance GABA-A by inc FREQUENCY of Cl channel opening

Front 45

Clinical uses of BENZOS?

Back 45

anxiety, spasticity, detox (esp etoh), night terrors, sleepwalking, 1st line status epilepticus (lorazepam and diazepam)--also used to prevent seizures of eclampsia

Front 46

Tx for BENZO O.D.?

Back 46

FLUMAZENIL (competitive agonist at GABA receptor)

Front 47

name BENZOS

Back 47

DIAZEPAM, LORAZEPAM, TRIAZOLAM, TEMAZEPAM, OXAZEPAM, MIDAZOLAM, CHLORDIAZEPOXIDE, ALPRAZOLAM

Front 48

short acting BENZOS?

Back 48

TRIAZOLAM, OXAZEPAM, MIDAZOLAM
(TOM thumb)

Front 49

name inhaled anesthetics

Back 49

HALOTHANE, ENFLURANE, ISOFLURANE, SEVOFLURANE, METHOXYFLURANE, NITROUS OXIDE

Front 50

how does potency of inhaled anesthetics relate to lipid solubility?

Back 50

potency is directly proportional to lipid solubility

Front 51

clinical effects of inhaled anesthetics?

Back 51

myocard dep, resp dep, naus/emesis, inc cerebral blood flow (dec cerebral metabolic demand)

Front 52

SE/toxicity of inhaled anesthetics?

Back 52

malig hyperthermia (w/gen predisp, causes massive release of Ca stores, tonic musc contrac); hepatotox (HALOTHANE); nephrotox (METHOXYFLURANE); proconvulsant (ENFLURANE)

Front 53

what is the solubility and potency of NITROUS OXIDE? how does this impact is usage?

Back 53

used in conjunction w/others b/c can't produce complete anesth alone; low blood and lipid solubility, thus fast induction and low potency, which permits close regulation of the level of anesth; is also least likely to dec BP or inc pCO2

Front 54

classes of IV anesthetics?

Back 54

barbituates, benzos, ketamine (arylcylcohexamines), opiates, propofol

Front 55

name BARBITUATES

Back 55

PHENOBARBITAL, PENTOBARBITAL, THIOPENTAL, SECOBARBITAL

Front 56

time of onset on THIOPENTAL?

Back 56

unconsciousness 15-30sec after admin

Front 57

what characteristics are responsible for fast onset/short duration of THIOPENTAL?

Back 57

high pot, high lipid solubility (crosses BBB fast, but also has fast redistribution to other organs)

Front 58

clinical uses of THIOPENTAL?

Back 58

induction of anesth in combo w/inhaled anesth', often in short surgical procedures

Front 59

effect of THIOPENTAL on cerebral blood flow?

Back 59

it decreases cerebral blood flow and O2 consumption by brain

Front 60

what drug is most commonly used for endoscopy?

Back 60

MIDAZOLAM

Front 61

clinical indications for BENZOS

Back 61

pre-op sedation, intra-op sedation (if analgesia not required), in combo w/other agents

Front 62

why is MIDAZOLAM a good pre-op agent?

Back 62

it produces antegrade amnesia (loss of mem after admin of drug), which calms pt

Front 63

what type of anesthesia does KETAMINE produce?

Back 63

dissociative anesthesia (=catatonia, amnesia, analgesia w/o loss of consc)

Front 64

clinical indications of KETAMINE

Back 64

trauma cases where CV support needed; in kids during painful procedures, to facilitate pt coop

Front 65

CV effects of KETAMINE?

Back 65

stim' sympathetic NS -> CV stim (inc HR, art BP, CO)

Front 66

effects of KETAMINE on cerebral blood flow?

Back 66

INC' cerebral blood flow (thus is NOT used in head trauma cases)

Front 67

SEs of KETAMINE?

Back 67

halluc, bad dreams, disorientation

Front 68

name opioids used as IV anesthetics

Back 68

MORPHINE, FENTANYL

Front 69

MoA of MORPHINE

Back 69

binds mu-opioid recep -> dec NT release from presyn nocioceptive neurons, and hyperpol' and inhib' postsyn neurons

Front 70

clinical uses of MORPHINE?

Back 70

severe pain, acute pulm edema (venodil->dec preload->dec perception of SOB)

Front 71

SEs of MORPHINE?

Back 71

dependence, w/drawl, O.D., constipation (dec motility), biliary colic (inc sphincter of Oddi tone), naus/vom

Front 72

sx of OPIOID withdrawal?

Back 72

lacrimation, rhinorrhea, sweating, gooseflesh, nausea, tachypnea

Front 73

sx of OPIOID O.D.?

Back 73

coma, pinpoint pupils, resp dep

Front 74

tx for OPIOID O.D.?

Back 74

NALOXONE (=pure antag at opioid mu recep)

Front 75

uses of PROPOFOL?

Back 75

rapid anesth induction and short procedures (similar pharm-dynam as thiopental, but w/less postop nausea)

Front 76

what are the 2 types of local anesthetics?

Back 76

ester and amide anesthetics

Front 77

name ester anesthetics

Back 77

PROCAINE, COCAINE, TETRACAINE

Front 78

name amide anesthetics

Back 78

LIDOCAINE, MEPIVACAINE, BUPIVACAINE

Front 79

MoA of local anesthetics?

Back 79

block Na channels by binding on inside of membrane, thus block nerve conduc

Front 80

how does charge affect mech/binding of local anesthetics?

Back 80

tert amine local anesth' penetrate memb in uncharged form, bind as charged form

Front 81

what dosing adjustments must be made for local anesthetics when used on infected (acidic) tissue?

Back 81

must use more, b/c in acidic envir anesth' are charged and can't penetrate membrane effectively

Front 82

what is the order of nerve blockade by local anesthetics?

Back 82

rapidly firing>slowly; smaller>larger; myelinated>unmyel (less impt)

ex. very small unmyel pain fiber>small myel ANS fiber>large myel ANS fiber

Front 83

order of sensation loss with local anesthesia?

Back 83

pain>temp>touch>pressure

Front 84

what type of drug are local anesthetics commonly paired with? why?

Back 84

vasoconstrictors (alpha-1 agonist, eg. epi)-> enhance local action, inc duration of action (limits removal/metab of drug), dec bleeding

Front 85

clinical uses of local anesthetics?

Back 85

minor surg procedures, spinal anesthesia

Front 86

toxicity of local anesthetics?

Back 86

CNS excitation (restlessness, paresthesias, tinnitus, convulsions); myocard dep and hypotens, except cocaine, which causes vasocons and hypertens

Front 87

clinical uses of neuromuscular blocking drugs

Back 87

musc paralysis in surg or mechanical ventilation

Front 88

name depolarizing neuromusc blockers

Back 88

SUCCINYLCHOLINE

Front 89

MoA of SUCCINYLCHOLINE?

Back 89

PHASE 1 (prolonged depol): binds motor nicotinic recep, opens Na chan, memb depol, transient fasic'->flaccid paralysis

PHASE 2 (repolarized but blocked): memb partially repol', but is desens'd to ACh, preventing further APs

Front 90

Is there an antidote to SUCCINYLCHOLINE during PHASE 1 blockade?

Back 90

no

Front 91

what happens if give cholinesterase inhibitor during PHASE 1 SUCCINYLCHOLINE blockade?

Back 91

the block is potentiated by AChE inhib

Front 92

is there an antidote to PHASE 2 SUCCINYLCHOLINE blockade?

Back 92

yes: AChE inhib (eg neostigmine)

Front 93

name nondepolarizing neuromuscular blocking drugs

Back 93

TUBOCURARINE, ATRACURIUM, MIVACURIUM, PANCURONIUM, VECURONIUM, RAPACURONIUM

Front 94

MoA of nondepol neuromusc blockers?

Back 94

competitively block chol transmiss at nic recep by preventing ACh from binding to receptor

Front 95

can nondepol neuromusc block be reversed?

Back 95

yes: AChE inhibitors (eg neostigmine, edrophonium, etc)

Front 96

concomittant admin of what two drugs causes malignant hyperthermia?

Back 96

inhalation anesthetics (except N2O) and succinylcholine

Front 97

clinical uses of DANTROLENE?

Back 97

tx of malignant hyperthermia, and neuroleptic malignant syndrome

Front 98

MoA of DANTROLENE?

Back 98

prevents release of Ca from sarco retic of skel musc