Exam 5 Flashcards
(124 cards)
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
2
Q
Suppressants of acute gouty attack
A
NSAIDS, colchicine, corticosteroids
3
Q
Corticosteroids to treat gout
A
Prednisone, methylprednisolone
4
Q
Drugs to increase excretion of uric acid
A
Probenecid, sulfinpyrazone
5
Q
Drugs that inhibit the formation of uric acid
A
Allopurinol, febuxostat
6
Q
Drugs that facilitate uric acid breakdown
A
Rasbicurase, pegloticase
7
Q
Ketoralac
A
IM in tx of severe acute gout attacks
Widely used as analgesic
8
Q
Aspirin in tx of gout
A
Avoided because of biphasic effect on uric acid secretion
9
Q
Phenylbutazone
A
Bone marrow toxicity, taken off market
Successfully treats acute gout attacks
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
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
12
Q
Febuxostat
A
Inhibits Xanthine oxidase. Reduces formation of uric acid. Not for acute gout.
Causes fewer skin problems than allopurinol
High cost
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)
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
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
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
17
Q
Colbenimid
A
Combo product of probenecid and colchicine
18
Q
Preferred tx for ppl who do not excrete large amounts of uric acid
A
Probenecid, sulfinpyrazole
19
Q
Best drugs for those who are synthesizing excess uric acid..chemotherapy
A
Allopurinol, febuxostat
20
Q
Gout drugs for ppl with kidney stones
A
Allopurinol, febuxostat
21
Q
Refractory gout
A
Pegloticase, resburicase
22
Q
Best drug for severe acute gout attack
A
Ketorolac
23
Q
Tx of a symptomatic hyperuricemia
A
Allopurinol or uricosuric agent
Dietary/ lifestyle change
24
Q
Drugs that act at 5 HT receptors
A
Ergotamine tartrate, dihydroergotamine, sumatriptan, zolmitriptan
25
HT 1b/1d agonists
Sumatriptan, zolmitriptan
26
Dopamine antagonists-antiemetics (for headache)
Metoclopramide, prochlorperazine, chlorpromazine
27
Analgesics used to treat headaches
Aspirin, acetaminophen, ibuprofen
28
Beta blockers used to treat headaches
Propranolol, timolol, atenolol, metropolol, nadolol
29
Antidepressants used to treat headaches
Amitriptyline
30
Anticonvulsant drugs to treat headache
Valproate, topiramate, gabapentin
31
Treximet
Naproxen and sumatriptan
32
NSAIDS
Block prostaglandin synthesis which prevents inflammation In the trigeminovascular system
33
Acetaminophen
Treat migraine and symptoms such as photophobia, photophobia, and pain
34
Excedrin
Aspirin, acetaminophen, caffeine
35
Midrin
Isometheptene (vasoconstrictor), dichloralphenazone (sedative), acetaminophen
36
Prodrin
Isometheptene, caffeine, acetaminophen
37
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
38
Dihydroergotamine
Administered parentally
Stimulation of 5HT1 receptors-direct vasoconstriction of dilated intracranial arteries, reduced neurogenic inflammation
Less likely to cause vasospasm vs ergotamine
39
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)
40
Zolmitriptan
Only second generation triptan with nasal and oral formulations available.
41
Metoclopramide
Dopamine antagonist- Antiemetic used to tx headache pain and nausea associated
SE include akathisia, systolic rxns (tx with diphenydramine)
42
Prochlorperazine
Dopamine antagonist- Antiemetic used to tx headache pain and nausea associated
SE include akathisia, systolic rxns (tx with diphenydramine)
43
Chlorpromazine
Dopamine antagonist-Antiemetic used to tx headache pain and nausea associated
SE include akathisia, systolic rxns (tx with diphenydramine)
44
Acebutolol
Beta blocker partial agonist not appropriate for migraine prophylaxis.
45
Pindolol
Beta blockers with partial agonist activity not appropriate for migraine prophylaxis.
46
Propanolol
Beta blockers for migraine prophylaxis.
47
Nadolol
Beta blockers for migraine prophylaxis. Less CNS effects
48
Timolol
Beta blockers for migraine prophylaxis.
49
Atenolol
Beta blockers for migraine prophylaxis. Less CNS effects.
50
Metropolol
Beta blockers for migraine prophylaxis.
51
Amitriptyline
Tricyclics antidepressant used for migraine prophylaxis. Down regulates central 5HT2 and adrenergic receptors.
52
Nortiptyline
TCA prophylaxis for migraine with better side effect profile
53
Protriptyline
TCA prophylaxis for migraine with better side effect profile
54
Valproic acid
Anti epileptic drug for migraine prophylaxis. Mechanism: facilitates GABA neurotransmission, modulates glutamate, inhibits Na and Ca channels
55
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
56
Botulinum toxin type a
Effects up to 3 months
| Good in pts with medication rebound headaches
57
Acute tx of cluster
Oxygen inhalation, ergotamine tartrate, subQ sumatriptan
58
Acute tx of tension
OTC analgesics, relaxation techniques
59
Prophylaxis of cluster
Only during cluster period. Verapamil, lithium carbonate, ergotamine tartrate, prednisone
60
Prophylaxis of tension
Amitriptyline, botulinum toxin injection IM
61
Calcium channel blockers
Prophylaxis for migraine
62
phenobarbital
monotherapy for generalized tonic/clonic seizures and partial seizures
-IV to treat status epilepticus
increase GABA-A effects
63
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
64
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
65
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
66
ethosuximide
monotherapy for absence seizures
inhibits T-type Ca channels
-few drug drug interactions (not bound to proteins)
CAN CAUSE SJS
SE: aplastic anemia
67
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
68
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
69
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
70
pregabalin
Treatment of partial seizures
GABA molecule bound to isobutane
also treats fibromyalgia
71
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
72
topiramate
monotherapy and adjunctive therapy for partial and tonic/clonic and LGS
- Inhibits Na channels and AMPA kainate receptors
- enhances GABA receptors
73
levetiracetam
EXTREMELY SAFE
adjunctive treatment for partial and tonic/clonic seizures in adults, myoclonic seizures in kids
-can treat status epilepticus
presynaptic glutamate release?
74
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
75
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
76
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
77
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)
78
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)
79
ropinirole
preferentially targets D2/D3 receptors
| used in treatment of restless leg syndrome
80
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
81
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
82
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
83
entacapone
inhibits metabolism of DA and I-DOPA by COMT
| -allows for more stable level of I-DOPA
84
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
85
trihexyphenidyl
anti-muscarinic
- effective against tremor of parkinsonism
- drug of choice for drug induced parkinsonism from DA antagonists
- drug interaction with CNS depressants
86
diphenydramine
anti-cholinergic
| -effective in parkinsonism
87
Sinemet
Carbidopa plus I-DOPA
88
Carbergoline
Newer dopamine agonist that is approved to treat hyperprolactinemia
89
Stalevo
combo product that contains I-DOPA plus carbidopa plus entacapone
90
Essential tremor
propanolol, primidone, clonidine, gabapentin
91
ballismus
dopamine antagonists (haloperidol)
92
dystonia
anticholinergics, benzodiazepines, botulinum toxin
93
choriea
dopamine antagonists, benzodiazepines, cholinesterase inhibitors
94
Tic diosrders
dopamine antagonists (haloperidol)
95
Alprazolam
benzodiazepine-anxiolytic
| intermediate duration of action
96
Chlordiazepoxide
benzo-anxiolytic, anticonvulsant, withdrawl suppressant
long duration of action
ACTIVE METABOLITES
97
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
98
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
99
midazolam
benzo- induction of anesthesia
| -significant respiratory depression
100
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
101
triazolam
benzo-hypnotic
| short duration of action (better for ppl who have trouble falling asleep-doesn't decrease REM)
102
Flumezenil
Benzo antagonist
- REVERSES CNS depressant effects (surgical or poisoning)
- can trigger seizures
- symptoms of withdrawal in addicted ppl
103
butalbital
barbiturate
104
pentobarbital
barbiturate
105
phenobarbital
barbiturate-anticonvulsant
| -tx of epilepsy
106
thiopental
barbiturate
induction of anesthesia
-truth serum (no longer available)
ultra short acting-redistribution of drug terminates action
107
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,
108
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
109
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
110
metaxalone
muscle relaxant, similar to cyclobenzaprine
111
tizanidine
skeletal muscle relaxant, alpha 2 agonist
| -very sedating
112
alcohol
anxiolytic
113
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
114
gammahydroxybutyrate
ergogenic effect-enhancement of althletic performance
"date rape drug"
ANALOG of GABA that can cross BBB
Street drug
115
melatonin
hormone produced by pineal gland
| agonist at melatonin receptors (doesn't decrease REM)
116
ramelteon
melatonin agonist
potention for interactions at CYP1A2
can increase levels of PRL and decrease levels of testosterone
117
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
```
118
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
```
119
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
```
120
propofol
IV induction and maintenance of anesthesia
approved for use of continuous sedation in ICU
-rapid onset, short duration
-redistribution accounts for short duration
121
diphenhydramine
antihistamine that can be used to sedate
-mild sedative
(plus hydroxyzine, promethazine, methotrimeprazine)
122
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
123
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)
124
naltrexone
treatment of alcoholism-long acting opioid antagonist
- decrease craving for alcohol
- can cause hepatotoxicity-limit its use
