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Pharmacology > Exam 5 > Flashcards

Exam 5 Flashcards

1
Q

NSAIDS to treat gout

A

Indomethacin, ibuprofen, ketorolac (usually max dose needed)

Inhibit prostaglandin synthesis

GI irritation and indomethacin can cause CNS effects

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2
Q

Suppressants of acute gouty attack

A

NSAIDS, colchicine, corticosteroids

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3
Q

Corticosteroids to treat gout

A

Prednisone, methylprednisolone

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4
Q

Drugs to increase excretion of uric acid

A

Probenecid, sulfinpyrazone

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5
Q

Drugs that inhibit the formation of uric acid

A

Allopurinol, febuxostat

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6
Q

Drugs that facilitate uric acid breakdown

A

Rasbicurase, pegloticase

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7
Q

Ketoralac

A

IM in tx of severe acute gout attacks

Widely used as analgesic

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8
Q

Aspirin in tx of gout

A

Avoided because of biphasic effect on uric acid secretion

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9
Q

Phenylbutazone

A

Bone marrow toxicity, taken off market

Successfully treats acute gout attacks

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10
Q

Colchicine

A

Antiinflammatory activity specific for gout. Binds to Tubulin and prevents polymerization to microtubules.

Overdose: throat pain, bloody diarrhea, CNS depression

SE: agranulocytosis, anemia, alopecia, neuropathy

Less frequent doses given to prevent recurrence of attacks

Oral or IV (for acute). 0.5-1 mg every two hours

Effect of drug can be diagnostic of gout

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11
Q

Allopurinol

A

Inhibits Xanthine oxidase. Reduces formation of uric acid. Not for acute gout.

Oxypurinol is metabolite that has long half life and helpful for long term tx

May need to use acute gout drugs in addition initially (colchicine)

Liver enzymes may elevate
Allergic rxns in pts with Renal problems

Increases half life of probenecid and theophylline (bronchodilator)…decrease hepatic metabolism of drugs

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12
Q

Febuxostat

A

Inhibits Xanthine oxidase. Reduces formation of uric acid. Not for acute gout.

Causes fewer skin problems than allopurinol

High cost

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13
Q

Probenecid

A

Inhibits secretion and reabsorption of organic acids…uric acid (more is reabsorbed than secreted, overall excretion increase)

Overdose leads to CNS effects

Causes increased risk of kidney stones as concentration rises in tubular fluid. Contraindicated in patients with kidney stones. Patients must stay hydrated to reduce risk. Not for acute attacks

SE: salicylates interfere with effect.
Interferes with tubular secretion of other drugs
Inhibits biliary secretion of rifampin (relate to tb)

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14
Q

Sulfinpyrazone

A

Inhibits secretion and absorption of uric acid

Greater risk of GI side effects than for Probenecid

Risk of drug interactions due to displacement from plasma proteins

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15
Q

Rasburicase

A

Recombinant urate- oxidase/ uricase enzymes. Converts uric acid to allantoin ( inactive and soluble metabolite)

Approved for peds patients receiving anti cancer tx– expected to result in tumor lysis syndrome

IV infusion important slow over several hours

May be good for tophaceous gout

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16
Q

Pegloticase

A

Recombinant urate- oxidase/ uricase enzymes. Converts uric acid to allantoin ( inactive and soluble metabolite)

Approved for adult with severe refractory gout

IV infusion slow over several hours

May be good for tophaceous gout

High incidence of allergic rxns

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17
Q

Colbenimid

A

Combo product of probenecid and colchicine

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18
Q

Preferred tx for ppl who do not excrete large amounts of uric acid

A

Probenecid, sulfinpyrazole

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19
Q

Best drugs for those who are synthesizing excess uric acid..chemotherapy

A

Allopurinol, febuxostat

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20
Q

Gout drugs for ppl with kidney stones

A

Allopurinol, febuxostat

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21
Q

Refractory gout

A

Pegloticase, resburicase

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22
Q

Best drug for severe acute gout attack

A

Ketorolac

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23
Q

Tx of a symptomatic hyperuricemia

A

Allopurinol or uricosuric agent

Dietary/ lifestyle change

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24
Q

Drugs that act at 5 HT receptors

A

Ergotamine tartrate, dihydroergotamine, sumatriptan, zolmitriptan

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25
Q

HT 1b/1d agonists

A

Sumatriptan, zolmitriptan

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26
Q

Dopamine antagonists-antiemetics (for headache)

A

Metoclopramide, prochlorperazine, chlorpromazine

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27
Q

Analgesics used to treat headaches

A

Aspirin, acetaminophen, ibuprofen

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28
Q

Beta blockers used to treat headaches

A

Propranolol, timolol, atenolol, metropolol, nadolol

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29
Q

Antidepressants used to treat headaches

A

Amitriptyline

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30
Q

Anticonvulsant drugs to treat headache

A

Valproate, topiramate, gabapentin

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31
Q

Treximet

A

Naproxen and sumatriptan

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32
Q

NSAIDS

A

Block prostaglandin synthesis which prevents inflammation In the trigeminovascular system

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33
Q

Acetaminophen

A

Treat migraine and symptoms such as photophobia, photophobia, and pain

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34
Q

Excedrin

A

Aspirin, acetaminophen, caffeine

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35
Q

Midrin

A

Isometheptene (vasoconstrictor), dichloralphenazone (sedative), acetaminophen

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36
Q

Prodrin

A

Isometheptene, caffeine, acetaminophen

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37
Q

Ergotamine tartrate

A

For acute treatment of migraine.
Second line drug

Caffeine can be added to potentiate vasoconstriction and improve intestinal absorption

Activation of 5 HT1b, may also reduce neurogenic inflammation by decreasing release of neuropeptide transmitters

Can add metoclopramide do decrease GI SE

Erythromycin can cause ergot toxicity

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38
Q

Dihydroergotamine

A

Administered parentally
Stimulation of 5HT1 receptors-direct vasoconstriction of dilated intracranial arteries, reduced neurogenic inflammation

Less likely to cause vasospasm vs ergotamine

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39
Q

Sumatriptan

A

First line to tx migraine
Derivative of serotonin
Metabolized by MAO

Causes constriction of inflamed/dilated intracranial arteries. Inhibits release of proinflammatories.

Relieves nausea, photophobia, phonophobia

Should not be given IV

Interaction with 5HT1A receptors causes side effects (chest tightness, etc)

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40
Q

Zolmitriptan

A

Only second generation triptan with nasal and oral formulations available.

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41
Q

Metoclopramide

A

Dopamine antagonist- Antiemetic used to tx headache pain and nausea associated

SE include akathisia, systolic rxns (tx with diphenydramine)

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42
Q

Prochlorperazine

A

Dopamine antagonist- Antiemetic used to tx headache pain and nausea associated

SE include akathisia, systolic rxns (tx with diphenydramine)

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43
Q

Chlorpromazine

A

Dopamine antagonist-Antiemetic used to tx headache pain and nausea associated

SE include akathisia, systolic rxns (tx with diphenydramine)

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44
Q

Acebutolol

A

Beta blocker partial agonist not appropriate for migraine prophylaxis.

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45
Q

Pindolol

A

Beta blockers with partial agonist activity not appropriate for migraine prophylaxis.

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46
Q

Propanolol

A

Beta blockers for migraine prophylaxis.

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47
Q

Nadolol

A

Beta blockers for migraine prophylaxis. Less CNS effects

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48
Q

Timolol

A

Beta blockers for migraine prophylaxis.

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49
Q

Atenolol

A

Beta blockers for migraine prophylaxis. Less CNS effects.

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50
Q

Metropolol

A

Beta blockers for migraine prophylaxis.

51
Q

Amitriptyline

A

Tricyclics antidepressant used for migraine prophylaxis. Down regulates central 5HT2 and adrenergic receptors.

52
Q

Nortiptyline

A

TCA prophylaxis for migraine with better side effect profile

53
Q

Protriptyline

A

TCA prophylaxis for migraine with better side effect profile

54
Q

Valproic acid

A

Anti epileptic drug for migraine prophylaxis. Mechanism: facilitates GABA neurotransmission, modulates glutamate, inhibits Na and Ca channels

55
Q

Topiramate

A

Side effects: parathesia, fatigue, anorexia, weight loss, memory loss

Anti epileptic drug for migraine prophylaxis. Mechanism: facilitates GABA neurotransmission, modulates glutamate, inhibits Na and Ca channels

56
Q

Botulinum toxin type a

A

Effects up to 3 months

Good in pts with medication rebound headaches

57
Q

Acute tx of cluster

A

Oxygen inhalation, ergotamine tartrate, subQ sumatriptan

58
Q

Acute tx of tension

A

OTC analgesics, relaxation techniques

59
Q

Prophylaxis of cluster

A

Only during cluster period. Verapamil, lithium carbonate, ergotamine tartrate, prednisone

60
Q

Prophylaxis of tension

A

Amitriptyline, botulinum toxin injection IM

61
Q

Calcium channel blockers

A

Prophylaxis for migraine

62
Q

phenobarbital

A

monotherapy for generalized tonic/clonic seizures and partial seizures

-IV to treat status epilepticus

increase GABA-A effects

63
Q

phenytoin

A

monotherapy for tonic/clonic and partial seizures

Blocks voltage gated Na channels

CYP3A4 activation causes increased metabolism of oral contraceptives

SE include gingival hyperplasia, SJS

64
Q

carbamazepine

A

monotherapy for tonic/clonic and partial seizures

prolongs rate of recovery of voltage gated Na channels
and blocks Na channels
-metabolized to 10,00 epoxide, which is just as effective
-increased metabolism of oral contraceptives

65
Q

oxcarbazepine

A

monotherapy OR adjunctive for partial seizures

blocks voltage gated Na channels and prolongs rate of channel recovery

  • prodrug that is converted to active metabolite in liver
  • inactivated by glucoronide conjugation
  • SE: increased metabolism of oral contraceptives
66
Q

ethosuximide

A

monotherapy for absence seizures

inhibits T-type Ca channels
-few drug drug interactions (not bound to proteins)
CAN CAUSE SJS
SE: aplastic anemia

67
Q

valproic acid

A

monotherapy for absence, myoclonic, partial, tonic/clonic

prolongs inacivation of Na channels, incrases GABA synthesis in vitro, inhibits T-type Ca channels

-BROAD SPECTRUM AED

inhibits CYP2C9-increases concentrations of phenytoin and phenobarbital

SE: can decrease IQ in children exposed in utero

68
Q

benzos in seizure treatment

A

clonazepam, clorazepate

TX OF ABSENCE SEIZURES and juvenile myoclonic seizures (synaptic inhibition via GABA-A receptors)

withdrawl can lead to status epilepticus

69
Q

gabapentin

A

GABA molecule bound to hexane ring (doesnt interact at GABA, but suppresses neuronal activity)
Binds to L-type Ca channels

-excreted unchanged in urine: TEST creatinine clearance prior to dosing

70
Q

pregabalin

A

Treatment of partial seizures
GABA molecule bound to isobutane

also treats fibromyalgia

71
Q

Lamotrigine

A

monotherapy/adjunctive for partial and generalized tonic/clonic seizures, LGS!!!

prolongs recovery of voltage gated Na channels from inactivation, inhibits Ca to a lesser extent

72
Q

topiramate

A

monotherapy and adjunctive therapy for partial and tonic/clonic and LGS

  • Inhibits Na channels and AMPA kainate receptors
  • enhances GABA receptors
73
Q

levetiracetam

A

EXTREMELY SAFE
adjunctive treatment for partial and tonic/clonic seizures in adults, myoclonic seizures in kids
-can treat status epilepticus

presynaptic glutamate release?

74
Q

I-DOPA

A

converted to dopamine by DOPA decarboxylase
full effect takes 3-4 weeks
less effective as disease progresses.
nausea due to CRTZ stimulation by dopamine
-clozapine can manage psych side effects

Drug interactions

  • pyridoxine (vit b6) enchances drug metabolism
  • antpsych drugs inhibit effect
  • MAO inhibitors and TCA’s cause hypertension
75
Q

I-DOPA plus carbidopa

A

Carbidopa-peripheral DOPA decarboxylase inhibitor (doesn’t enter brain)–>decreases side effects

converted to dopamine by DOPA decarboxylase
full effect takes 3-4 weeks
less effective as disease progresses.
nausea due to CRTZ stimulation by dopamine
-clozapine can manage psych side effects

Drug interactions

  • pyridoxine (vit b6) enchances drug metabolism
  • antpsych drugs inhibit effect
  • MAO inhibitors and TCA’s cause hypertension
76
Q

I-DOPA plus carbidopa and entacapone

A

Entacapone-inhibits metabolsim of dopamine adn I-DOPA by COMT–>more sustained level of drug

Carbidopa-peripheral DOPA decarboxylase inhibitor (doesn’t enter brain)–>decreases side effects

converted to dopamine by DOPA decarboxylase
full effect takes 3-4 weeks
less effective as disease progresses.
nausea due to CRTZ stimulation by dopamine
-clozapine can manage psych side effects

Drug interactions

  • pyridoxine (vit b6) enchances drug metabolism
  • antpsych drugs inhibit effect
  • MAO inhibitors and TCA’s cause hypertension
77
Q

bromocriptine

A

Ergot derivative-non specific DA receptor agonist

  • decreased severity of on/off phenomenon
  • less effective than I-DOPA
  • inhibits prolactin secretion (can be used to treat amenorrhea and galactorrhea-but no longer approved)
78
Q

pramipexole

A

preferentially targets D2/D3 receptors
used in treatment of restless leg syndrome
-may have antioxidant and neuroprotective effects in slowing progression of disease
(argued that it should be drug of choice for initial tx)

79
Q

ropinirole

A

preferentially targets D2/D3 receptors

used in treatment of restless leg syndrome

80
Q

amantadine

A

originally antiviral

  • stimulates release of dopamine from nerve endings
  • less effective than I-DOPA in tx of parkinsonism, but better than anticholinergics
  • requires dosage adjustment in pts with impaired renal function
81
Q

selegiline/deprenyl

A

inhibits MAO-B and prevents breakdown of DA in CNS

  • do not interact with tyramine
  • may decrease the severity of on-off phenomenon in I-DOPA
  • “cheese toxicity” at high doses, weight loss and nausea
82
Q

Rasagiline

A

Newer, more powerful drug approved for use in early and late stages of Parkinsons disease
inhibits MAO-B and prevents breakdown of DA in CNS
-“cheese toxicity” at high doses, weight loss, nausea

83
Q

entacapone

A

inhibits metabolism of DA and I-DOPA by COMT

-allows for more stable level of I-DOPA

84
Q

benztropine

A

anti-muscarinic

  • effective against tremor of parkinsonism
  • drug of choice for drug induced parkinsonism from DA antagonists
  • drug interaction with CNS depressants
  • some ability to inhibit synaptic reuptake of DA
85
Q

trihexyphenidyl

A

anti-muscarinic

  • effective against tremor of parkinsonism
  • drug of choice for drug induced parkinsonism from DA antagonists
  • drug interaction with CNS depressants
86
Q

diphenydramine

A

anti-cholinergic

-effective in parkinsonism

87
Q

Sinemet

A

Carbidopa plus I-DOPA

88
Q

Carbergoline

A

Newer dopamine agonist that is approved to treat hyperprolactinemia

89
Q

Stalevo

A

combo product that contains I-DOPA plus carbidopa plus entacapone

90
Q

Essential tremor

A

propanolol, primidone, clonidine, gabapentin

91
Q

ballismus

A

dopamine antagonists (haloperidol)

92
Q

dystonia

A

anticholinergics, benzodiazepines, botulinum toxin

93
Q

choriea

A

dopamine antagonists, benzodiazepines, cholinesterase inhibitors

94
Q

Tic diosrders

A

dopamine antagonists (haloperidol)

95
Q

Alprazolam

A

benzodiazepine-anxiolytic

intermediate duration of action

96
Q

Chlordiazepoxide

A

benzo-anxiolytic, anticonvulsant, withdrawl suppressant
long duration of action
ACTIVE METABOLITES

97
Q

diazepam

A

benzo-anxiolytic, anticonvulsant, anesthesia supplement, withdrawl suppressant, muscle relaxant
long duration of action
ACTIVE METABOLITES
(less intense of a withdrawl but lasts longer)
duration changes when given acutely or chronically

98
Q

lorazepam

A

benzo-hypnotic, anxiolytic, anesthesia supplement, withdrawl suppressant
intermediate duration of action
NO ACTIVE METABOLITES
-does not use oxidation pathway-good for ppl with bad livers

99
Q

midazolam

A

benzo- induction of anesthesia

-significant respiratory depression

100
Q

temazepam

A

benzo-hypnotic (can be used to help ppl sleep)
intermediate duration of action
-can help for ppl who have troubles with waking up during sleep

101
Q

triazolam

A

benzo-hypnotic

short duration of action (better for ppl who have trouble falling asleep-doesn’t decrease REM)

102
Q

Flumezenil

A

Benzo antagonist

  • REVERSES CNS depressant effects (surgical or poisoning)
  • can trigger seizures
  • symptoms of withdrawal in addicted ppl
103
Q

butalbital

A

barbiturate

104
Q

pentobarbital

A

barbiturate

105
Q

phenobarbital

A

barbiturate-anticonvulsant

-tx of epilepsy

106
Q

thiopental

A

barbiturate
induction of anesthesia
-truth serum (no longer available)
ultra short acting-redistribution of drug terminates action

107
Q

balcofen

A

Cenrally acting muscle relaxant-GABA analog-acts as agonist at GABA-B (inhibit release of glutamate and aspartate)
used to treat spasticity d/t MS, spinal cord injuries,

108
Q

cyclobenzaprine

A

Centrally acting muscle relaxant-treat muscle spasms of local origin (strains)
-related to tricyclic antidepressants-acts at brainstem to inhibit both gamma and alpha motor systems

109
Q

diazepam

A

centrally acting muscle relaxant (benzo)-treat spasticity and muscle spasms

  • enhances presynaptic inhibition by facilitating actions of GABA
  • more lipid soluble
  • half life changes when given acutely vs. chronically
110
Q

metaxalone

A

muscle relaxant, similar to cyclobenzaprine

111
Q

tizanidine

A

skeletal muscle relaxant, alpha 2 agonist

-very sedating

112
Q

alcohol

A

anxiolytic

113
Q

buspirone

A

alleviates anxiety with minimal other effects
-takes 1-2 weeks before kicks in (low abuse potential)
-no cross tolerance or dependence with other abused drugs
ANXIETY IN ALCOHOLICS (but not for symptoms of withdrawal)
-partial agonist at serotonin (5HT1A) receptors
significant first pass metabolism
INTERACTIONS with MAO inhibitors, cimetidine, antidepressants and antipsychotics

114
Q

gammahydroxybutyrate

A

ergogenic effect-enhancement of althletic performance
“date rape drug”
ANALOG of GABA that can cross BBB
Street drug

115
Q

melatonin

A

hormone produced by pineal gland

agonist at melatonin receptors (doesn’t decrease REM)

116
Q

ramelteon

A

melatonin agonist
potention for interactions at CYP1A2
can increase levels of PRL and decrease levels of testosterone

117
Q

eszopiclone

A 
non-benzo sedative hypnotic (new)
Less REM EFFECTS
bind to benzo receptors
less general effects compared to benzos
-enhance effects of GABA by interacting with omega 1 site)
potential for drug interactions
abuse less than benzos
interations with other CNS depressants
LONGER ACTING
118
Q

zolpidem

A 
LONGER ACTING
more side effects (complex behaviors while asleep)
non-benzo sedative hypnotic (new)
Less REM EFFECTS
bind to benzo receptors
less general effects compared to benzos
-enhance effects of GABA by interacting with omega 1 site)
potential for drug interactions
abuse less than benzos
interations with other CNS depressants
119
Q

zaleplon

A 
SHORTER ACTING
non-benzo sedative hypnotic (new)
Less REM EFFECTS
bind to benzo receptors
less general effects compared to benzos
-enhance effects of GABA by interacting with omega 1 site)
potential for drug interactions
abuse less than benzos
interations with other CNS depressants
120
Q

propofol

A

IV induction and maintenance of anesthesia
approved for use of continuous sedation in ICU
-rapid onset, short duration
-redistribution accounts for short duration

121
Q

diphenhydramine

A

antihistamine that can be used to sedate
-mild sedative
(plus hydroxyzine, promethazine, methotrimeprazine)

122
Q

disulfiram

A

drug to treat alcoholism

  • pt on med who consumes alcohol: flushing, headache, nausea, confusion (unpleasant)
  • INHIBITOR of ALDEHYDE DEHYDROGENASE-blocks conversion of acetaldehyde to acetate
  • if non compliant, can cause hepatotoxicity and drug interactions
123
Q

acamaprosate

A

treatment of alcoholism (new)
-decreases craving and helps maintain abstinence
-may involve actions at glutamate and GABA receptors
blocks NMDA receptors and stimulates GABA-A receptors
-less potential for hepatotoxicity (preferred drug for ppl with liver problems)
(naltrexone plus acomprostate may be best combo)

124
Q

naltrexone

A

treatment of alcoholism-long acting opioid antagonist

  • decrease craving for alcohol
  • can cause hepatotoxicity-limit its use

Pharmacology (6 decks)

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