Exam 5 Flashcards
NSAIDS to treat gout
Indomethacin, ibuprofen, ketorolac (usually max dose needed)
Inhibit prostaglandin synthesis
GI irritation and indomethacin can cause CNS effects
Suppressants of acute gouty attack
NSAIDS, colchicine, corticosteroids
Corticosteroids to treat gout
Prednisone, methylprednisolone
Drugs to increase excretion of uric acid
Probenecid, sulfinpyrazone
Drugs that inhibit the formation of uric acid
Allopurinol, febuxostat
Drugs that facilitate uric acid breakdown
Rasbicurase, pegloticase
Ketoralac
IM in tx of severe acute gout attacks
Widely used as analgesic
Aspirin in tx of gout
Avoided because of biphasic effect on uric acid secretion
Phenylbutazone
Bone marrow toxicity, taken off market
Successfully treats acute gout attacks
Colchicine
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
Allopurinol
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
Febuxostat
Inhibits Xanthine oxidase. Reduces formation of uric acid. Not for acute gout.
Causes fewer skin problems than allopurinol
High cost
Probenecid
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)
Sulfinpyrazone
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
Rasburicase
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
Pegloticase
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
Colbenimid
Combo product of probenecid and colchicine
Preferred tx for ppl who do not excrete large amounts of uric acid
Probenecid, sulfinpyrazole
Best drugs for those who are synthesizing excess uric acid..chemotherapy
Allopurinol, febuxostat
Gout drugs for ppl with kidney stones
Allopurinol, febuxostat
Refractory gout
Pegloticase, resburicase
Best drug for severe acute gout attack
Ketorolac
Tx of a symptomatic hyperuricemia
Allopurinol or uricosuric agent
Dietary/ lifestyle change
Drugs that act at 5 HT receptors
Ergotamine tartrate, dihydroergotamine, sumatriptan, zolmitriptan
HT 1b/1d agonists
Sumatriptan, zolmitriptan
Dopamine antagonists-antiemetics (for headache)
Metoclopramide, prochlorperazine, chlorpromazine
Analgesics used to treat headaches
Aspirin, acetaminophen, ibuprofen
Beta blockers used to treat headaches
Propranolol, timolol, atenolol, metropolol, nadolol
Antidepressants used to treat headaches
Amitriptyline
Anticonvulsant drugs to treat headache
Valproate, topiramate, gabapentin
Treximet
Naproxen and sumatriptan
NSAIDS
Block prostaglandin synthesis which prevents inflammation In the trigeminovascular system
Acetaminophen
Treat migraine and symptoms such as photophobia, photophobia, and pain
Excedrin
Aspirin, acetaminophen, caffeine
Midrin
Isometheptene (vasoconstrictor), dichloralphenazone (sedative), acetaminophen
Prodrin
Isometheptene, caffeine, acetaminophen
Ergotamine tartrate
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
Dihydroergotamine
Administered parentally
Stimulation of 5HT1 receptors-direct vasoconstriction of dilated intracranial arteries, reduced neurogenic inflammation
Less likely to cause vasospasm vs ergotamine
Sumatriptan
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)
Zolmitriptan
Only second generation triptan with nasal and oral formulations available.
Metoclopramide
Dopamine antagonist- Antiemetic used to tx headache pain and nausea associated
SE include akathisia, systolic rxns (tx with diphenydramine)
Prochlorperazine
Dopamine antagonist- Antiemetic used to tx headache pain and nausea associated
SE include akathisia, systolic rxns (tx with diphenydramine)
Chlorpromazine
Dopamine antagonist-Antiemetic used to tx headache pain and nausea associated
SE include akathisia, systolic rxns (tx with diphenydramine)
Acebutolol
Beta blocker partial agonist not appropriate for migraine prophylaxis.
Pindolol
Beta blockers with partial agonist activity not appropriate for migraine prophylaxis.
Propanolol
Beta blockers for migraine prophylaxis.
Nadolol
Beta blockers for migraine prophylaxis. Less CNS effects
Timolol
Beta blockers for migraine prophylaxis.
Atenolol
Beta blockers for migraine prophylaxis. Less CNS effects.
Metropolol
Beta blockers for migraine prophylaxis.
Amitriptyline
Tricyclics antidepressant used for migraine prophylaxis. Down regulates central 5HT2 and adrenergic receptors.
Nortiptyline
TCA prophylaxis for migraine with better side effect profile
Protriptyline
TCA prophylaxis for migraine with better side effect profile
Valproic acid
Anti epileptic drug for migraine prophylaxis. Mechanism: facilitates GABA neurotransmission, modulates glutamate, inhibits Na and Ca channels
Topiramate
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
Botulinum toxin type a
Effects up to 3 months
Good in pts with medication rebound headaches
Acute tx of cluster
Oxygen inhalation, ergotamine tartrate, subQ sumatriptan
Acute tx of tension
OTC analgesics, relaxation techniques
Prophylaxis of cluster
Only during cluster period. Verapamil, lithium carbonate, ergotamine tartrate, prednisone
Prophylaxis of tension
Amitriptyline, botulinum toxin injection IM
Calcium channel blockers
Prophylaxis for migraine
phenobarbital
monotherapy for generalized tonic/clonic seizures and partial seizures
-IV to treat status epilepticus
increase GABA-A effects
phenytoin
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
carbamazepine
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
oxcarbazepine
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
ethosuximide
monotherapy for absence seizures
inhibits T-type Ca channels
-few drug drug interactions (not bound to proteins)
CAN CAUSE SJS
SE: aplastic anemia
valproic acid
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
benzos in seizure treatment
clonazepam, clorazepate
TX OF ABSENCE SEIZURES and juvenile myoclonic seizures (synaptic inhibition via GABA-A receptors)
withdrawl can lead to status epilepticus
gabapentin
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
pregabalin
Treatment of partial seizures
GABA molecule bound to isobutane
also treats fibromyalgia
Lamotrigine
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
topiramate
monotherapy and adjunctive therapy for partial and tonic/clonic and LGS
- Inhibits Na channels and AMPA kainate receptors
- enhances GABA receptors
levetiracetam
EXTREMELY SAFE
adjunctive treatment for partial and tonic/clonic seizures in adults, myoclonic seizures in kids
-can treat status epilepticus
presynaptic glutamate release?
I-DOPA
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
I-DOPA plus carbidopa
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
I-DOPA plus carbidopa and entacapone
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
bromocriptine
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)
pramipexole
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)
ropinirole
preferentially targets D2/D3 receptors
used in treatment of restless leg syndrome
amantadine
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
selegiline/deprenyl
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
Rasagiline
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
entacapone
inhibits metabolism of DA and I-DOPA by COMT
-allows for more stable level of I-DOPA
benztropine
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
trihexyphenidyl
anti-muscarinic
- effective against tremor of parkinsonism
- drug of choice for drug induced parkinsonism from DA antagonists
- drug interaction with CNS depressants
diphenydramine
anti-cholinergic
-effective in parkinsonism
Sinemet
Carbidopa plus I-DOPA
Carbergoline
Newer dopamine agonist that is approved to treat hyperprolactinemia
Stalevo
combo product that contains I-DOPA plus carbidopa plus entacapone
Essential tremor
propanolol, primidone, clonidine, gabapentin
ballismus
dopamine antagonists (haloperidol)
dystonia
anticholinergics, benzodiazepines, botulinum toxin
choriea
dopamine antagonists, benzodiazepines, cholinesterase inhibitors
Tic diosrders
dopamine antagonists (haloperidol)
Alprazolam
benzodiazepine-anxiolytic
intermediate duration of action
Chlordiazepoxide
benzo-anxiolytic, anticonvulsant, withdrawl suppressant
long duration of action
ACTIVE METABOLITES
diazepam
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
lorazepam
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
midazolam
benzo- induction of anesthesia
-significant respiratory depression
temazepam
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
triazolam
benzo-hypnotic
short duration of action (better for ppl who have trouble falling asleep-doesn’t decrease REM)
Flumezenil
Benzo antagonist
- REVERSES CNS depressant effects (surgical or poisoning)
- can trigger seizures
- symptoms of withdrawal in addicted ppl
butalbital
barbiturate
pentobarbital
barbiturate
phenobarbital
barbiturate-anticonvulsant
-tx of epilepsy
thiopental
barbiturate
induction of anesthesia
-truth serum (no longer available)
ultra short acting-redistribution of drug terminates action
balcofen
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,
cyclobenzaprine
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
diazepam
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
metaxalone
muscle relaxant, similar to cyclobenzaprine
tizanidine
skeletal muscle relaxant, alpha 2 agonist
-very sedating
alcohol
anxiolytic
buspirone
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
gammahydroxybutyrate
ergogenic effect-enhancement of althletic performance
“date rape drug”
ANALOG of GABA that can cross BBB
Street drug
melatonin
hormone produced by pineal gland
agonist at melatonin receptors (doesn’t decrease REM)
ramelteon
melatonin agonist
potention for interactions at CYP1A2
can increase levels of PRL and decrease levels of testosterone
eszopiclone
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
zolpidem
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
zaleplon
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
propofol
IV induction and maintenance of anesthesia
approved for use of continuous sedation in ICU
-rapid onset, short duration
-redistribution accounts for short duration
diphenhydramine
antihistamine that can be used to sedate
-mild sedative
(plus hydroxyzine, promethazine, methotrimeprazine)
disulfiram
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
acamaprosate
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)
naltrexone
treatment of alcoholism-long acting opioid antagonist
- decrease craving for alcohol
- can cause hepatotoxicity-limit its use
