BMB Pharm

Question 1

First barbiturate used?

Answer 1

Phenobarbital, but rarely used now due to high risk for OD and abuse (usu rx benzos instead)

Question 2

Which NT channels sys do barbs/benzos act on?

Answer 2

Benzos increase opening of GABA channels, barbs increase length of opening
(barbs also inhib glu/ block Na)

Question 3

what do barbs do to benzo effects

Answer 3

incr affinity of GABA R channel for benzos so synergistic

Question 4

what happens when increasing dose of benzos vs barbiturates

Answer 4

same effect at low dose, but as dosing incr benzos level off while barbs can cause medullary coma etc (so benzos used more ,also good rescue drug bc fast acting)

Question 5

therapeutic indications of benzos and barbs?

Answer 5

anxiety, anticonvulsant (high doses, most barbs eg clonazepam and pheno), muscle relaxation (high doses, at low doses diazepam depresses SC reflexes to tx cerebral palsy/spastic), alc withdrawal

Question 6

what do you give to pts with alc withdrawal? what about liver failure? adv?

Answer 6

large dose of benzos in rehab, maybe barb, have good cross tolerance, anticonvl, not much resp depr
-for liver failure give lorezepam or oxazepam (since other are met in liver)

Question 7

What are the undesirable effects of benzos and barbs?

Answer 7

medullary depr, resp and CV collapse (esp barbs)
Tolerance and dependence, can get withdrawal like tremors or seizures
Psychomotor impairment (clumsy), Beh disinhibition,, amnesia

Question 8

Bispirone is another drug for treating?
what does it do?
Adv/ disadv?

Answer 8

anxiety
5HT1a partial agonist
-non sedative, no drug dependence risk, used for GAD or history of drug abuse
-but LONG onset!

Question 9

SSRI/SNRI tx anxiety adv/disadv?

Answer 9

common tx, but slow onset of action! but low risk of abuse

Question 10

Insomnia drugs
examples
sxe and counteract

Answer 10

Z drugs (benzo-like a1 selective agonists)
Melatonin agonists
Antihistamine/ TCA
Dual orexin receptor antag

Question 11

Z drugs for insomnia

Answer 11

Z drugs (benzo-like a1 selective agonists) most commonly rx, produce pure sedation without anxiolytic/anticonv/muscle

• only bind to GABA R channels with A1 receptor, incr total sleep time
• ex: Zolpidem (ambien), Zaleplon (sonata), Eszopicione (Lunesta)
• sxe: sleepwalking, amenesia, stronger w women, countneract with flumazenil

Question 12

Melatonin agonist

Answer 12

ramelteon rozerum, good for circadian rhythm issues

Question 13

antihistamine/TCA

Answer 13

Dopexin (silenor)

Question 14

dual orexin receptor antagonist and cxi

Answer 14

eg SUVOREXANT (belsomra), antagonizes the orexin (wakefulness) receptor, decr time to sleep onset so incr sleep maintenence
-CxI in narcolepsy