Pharm 1 Flashcards
1
Q
Barbiturates
A
- insomnia drug
- MOA: bind to and increase GABA actions
- AE: sedation –> hypnosis –> anesthesia –> coma
- not as safe as benzodiazepines
2
Q
Benzodiazepines
A
- insomnia drug
- MOA: modulates alpha subunit of GABA receptors, shifts dose-response curve to the left (allosteric modulation)
- conjugation and renal excretion
- AE: sedation, cognitive impairment, rebound insomnia, causes withdrawal (anxiety, irritatilbity, resp depression)
- schedule 4, category X
- contra: liver dz, COPD, depression, driving, other CNS depressants, glaucoma
3
Q
BZ 1-3 alpha receptor subgroup
A
BZ1 - sedation/amnesia
BZ2 - anxiolysis
BZ3 - myorelaxation/anticonvulsant
4
Q
Estazolam
A
- benzodiazepine for insomnia
- CYP3A4, doesn’t accumulate
- quick elim, short t1/2
5
Q
Flurazepam
A
- benzodiazepine for insomnia
- CYP3A4, does accumulate
6
Q
Quazepam
A
- benzodiazepine for insomnia
- CYP2D6>CYP3A4, accumulates
7
Q
Temazepam
A
- benzodiazepine for insomnia
- no cyps (conjugation)!! doesn’t accumulate
8
Q
Triazolam
A
- benzodiazepine for insomnia
- CYP3A4, no accumulation (rapidly inactivated)
9
Q
Benzodiazepine receptor agonist
A
- for insomnia
- similar MOA as benzos but safer
- AE: sedation, cog impairment, rebound insomnia, withdrawal (anxiety, irritability, restlessness, sleep apnea, resp depression)
- schedule 4, CYP interactions
- category C
- contra liver dz, COPD, depression, CNS drugs
10
Q
Zolpidem
A
- for insomnia
- aka Ambien
- benzo receptor agonist
- most prescribed hypnotic
- can get as sublingual (only one that can be used in middle of night) and oral spray
- use lower dose in women
11
Q
Zaleplon
A
- for insomnia
- benzo receptor agonist
- ald dehydrogenase
- variable dose in Asians
12
Q
Eszopiclone
A
Benzo receptor agonist for insomnia
13
Q
Flumazenil
A
- benzo antagonist to reverse effects of benzos/benzo agonists
- IV quick acting
- can cause abrupt awakening with dysphoria, agitation, can cause seizures, withdrawal
14
Q
Melatonin
A
- made in pineal gland, produces drowsiness involved in circadian rhythm
- GPCRs
- MT1 - attenuates SCN activity (sleepy)
- MT2 - maintains circadian rhythms
- MT3 not involved in sleeep
15
Q
Ramelteon
A
- melatonin receptor agonist, not scheudled
- no morning impairment, abuse, or resp depression
- AE: HA, somnolence, nausea, insomnia, URTI, nasopharyngiitis
16
Q
Antidepressants
A
- can be used for insomnia but not intended
- AE of sedation
- int with CYPs, other depressants, EtOH, BBW for suicide
17
Q
Doxepin
A
- antidepressant that can be used for insomnia
- primarily anti H1 at low doses
- SE: sedation, muscarinic blocker, SNRI
- the only one that’s actually approved
18
Q
Mirtazapine
A
- antidepressant that can be used for insomnia
- primarily alpha 2 antagonism (reinforces 5HT and NE release)
19
Q
Trazodone
A
- antidepressant that can be used for insomnia
- sedation with a little 5HTRI
20
Q
1st gen antihistamines
A
- for insomnia
- cross BBB, produce sedation through anti H1
- AE: zerostomia, blurred vision, urinary retention (anticholinergic), inc. ocular P
- rapid tolerance can develop
21
Q
Diphenhydramine and doxylamine
A
- 1st gen antihistamines for insomnia
22
Q
GABA receptor
A
a GPCR that gates entry of Cl- ions into cell
23
Q
At really high doses, ______ can actually activate and open the GABA channel on their own
A
barbiturates
24
Q
Tension headache tx
A
pts usually self medicate with NSAIDs (Ibuprofen, Naproxen)
25
Cluster headache tx
nasal/SC triptans or ergots
| steroids (prednisone)
26
for mild/moderate menstrual HA
give NSAIDs
27
for moderate/severe HA
give short acting triptan (Sumatriptan)
28
Prophylaxis of migraine
AMITRYPTILLINE - TCA/SNRI/antichol, ae aggresion/wt gain/xerostomia/sedation
TOPIRAMATE - blocks Na and glutamate/ inc GABA, ae parasthesia/nausea/fatigue/narrow therapeutic range
VALPROATE - Na channel blocker, inc GABA, CatX, hepatotoxic, highly protein bound
PROPANOLOL AND TIMOLOL - dec vasodilation, dec NE induced lipolysis, ae fatigue/asthma/DM/AV block/exercise intolerance
METOPROLOL
BOTOX - no vascular or systemic effect
29
Pregnancy and HA meds
- never Ergots
- acetometophen in 1st TM
- add opiods later if needed
- no NSAIDs in 3rd TM
30
Migraine and OCPs
- OCPs inc stroke risk
| - migraine with aura also inc stroke risk
31
NSAID DDIs
diuretics
b blockers
vasodilators (a2 agonists, a1 blockers)
32
What should you worry about with acetometophen?
G6PD deficiency - b/c depleted glutathione can cause rbi oxidative damage and result in anemia
33
Butalbital
- Barbiturate for HAs
- GABA sedative
- strongly linked to overuse syndrome
- cyp metab
34
Caffeine
- for HA
- causes vasoconstriction
- watch out for your hearrt
35
Triptans
- for HA
- selective 5HT1 B (blood vessels) and 5HT1 D (nerve terminals) --> dec release of CGRP and Substance P
- AE: worst with SC sumotriptan, chest pain, coronary vasospasm, contra heart dz/ischemic bowel disease/diabetes
- don't use within 24 hours: ergots, MAOIs, propanolol, CYP3A4 drugs, SSRI
36
The slowest triptan
Frovatriptan (Frova is slowa)
37
Ergots Alkaloids
- for HA
- cause vasoconstriction of small arteries
- acts on lots of receptors so lots of DDIs: b blockers, dopa, no triptans for 24h
- Cat X
- contra HTN, vascular dz, sepsis, MI
38
Ergotamine
- ergot for HAs
| - available as oral/suppository
39
Dihydroergotamine
- ergot for HAs
| - available as SC, IV, nasal spray
40
Anti-emetics
- for HAs
| - act on dopamine in the floor of the 4th ventricle and ACh in the vestibular system
41
Metoclopromide
- anti emetic for HA that is a central D2 blocker
- prokinetic in stomach
- inc. prolactin
42
Prochlopermazine
- anti emetic for HA that acts on D2 blocker
- also cholinergic/alpha adrenergic blocker
- AE: opp of SLUDGEBBB, glaucoma, dyskinesia, BPH
43
Chlorpromazine
- anti emeetic for HA that acts on D2 blocker
- also cholinergic and alpha adrenergic blocker
- AE: opp of SLUDGEBBB, glaucoma, dyskinesia, BPH
44
Promethazine
- anti emetic for HA that acts on cholinergic blockade
- anti H1 and weak D2 blocker
- parkinsonsm, opp of sludge BBB, BPH
45
the only drug approved for pediatric migraine prophylaxis
propanolol
46
General tx for brain tumors
steroids (dec. edema)
anticonvulsants
surgery!!
chemo (hard b/c of BBB)
47
resistance mechanisms of brain tumors
dec. drug uptake
dec. drug activation
inc. drug metabolism/efflux
repair of drug induced DNA damage
binding site alteration
inc. sulhydryl scavengers
alteration of target proteins (BCL2)
48
Temozolomide
- Label: Astrocytoma/GBM, Off: malignant glioma/melanoma
- prodrug DNA methylator
- oral/IV
- AE: myelosuppression, leukopenia, N/V, chills....CAT X
- resistance: tumor cells that express 06-MGMT (which hematopoeitic cells have low of :( )
49
Carmustine
- Nitrosurea for astrocytoma, mets, malignant gioma, medullo-
- DNA alkylator with low cross resistance
- very lipophilic (crosses BBB)
- AE: usuals + pulm fibrosis, endorcrine dysfunction (inc. PRL, dec. T3/T4), encephalopathy, seizures, dementia, inc. LFTs
- also carbamoylates (inh DNA repair)
- parenteral, implants as a wafer
50
Lomustine
- Nitrosurea for malignant glioma
- DNA alkylator with low cross resistance
- very lipophilic (crosses BBB)
- AE: usuals + pulm fibrosis, endocrine dysfunction (inc. PRL, dec. T3/T4), encephalopathy, seizures, dementia, inc. LFTs
- given oraly
51
Convection enhanced delivery
- delivering chemo and viral vectors via infusion with a positive pressure catheter
- still in clinical trials
52
Chemo fog
- long term AE of chemo
- damage to hippo, amyg, cerebellum
- maybe from inc. TNFalpha which can cross the BBB and damage mitochondria
