Sedatives and Hypnotics

Question 1

Neurotransmitters that plays important role in sleep or hypnotic actions?

Answer 1

GABA, histamine, Acetylcholine, Catecholamine, Adenosine

Question 2

Long acting BZDs undergo what type of metabolism?

Answer 2

Dia, Flu, Clo and Chlor = Dealkylation

Question 3

Short and intermediate acting BZDs undergo what type of metabolism?

Answer 3

Alpra, Tria = Oxidation

SA: Mid Tria = no phase I or extra hepatic metabolism

Question 4

Intermediate acting BZDs Lora Oxa Tema have short life due?

Answer 4

OH group at position 3 that undergoes phase II glucuronidation conjugation

Question 5

BZD without OH group at position 3 accounts for?

Answer 5

Its long half life, undergoes phase 1 hydroxylation reaction then phase II metabolism.

Question 6

BZD binds to what receptors and explain pharmacology.

Answer 6

BZ1 BZ2, parallel to GABA= increases channel opening, increase inhibitory effect of GABA on neuronal excitability

Question 7

Prodrug of Phenobarbital (active metabolite)

Answer 7

Primedone

Question 8

SAR. What is essential for sedative hypnotic activity?

For long activity?

Answer 8

• Two side chains in position 5

- Phenyl and Ethyl group in position 5

Question 9

Barbiturates. Ultra-short action, short acting, long action

Answer 9

USA: Thiopental
SA: Amo, Seco, Pentobarbital
LA: Phenobarbital

Question 10

BZD short and long term SEs

Answer 10

Short: become ineffective, causes memory loss, more irritable and less able to concentrate
Long: Drowsiness, tolerance dependency

Question 11

Barb pharmacology.

Answer 11

They interfere with Na and K transport across membrane potentiates GABA action on Cl entry.

Question 12

Examples of Non BZD GABA-A Agonists

Answer 12

Imidazopyridines: Zopiclone, Zolpidem, Pyrazolopyridine, Zeloplon

Question 13

Phenobarbitals are structurally related to what drugs? And sometimes used together.

Answer 13

Phenytoins

-and Primidone