Anxiolytic and Hypnotic Drugs

Question 1

What is the mechanism of Benzodiazepine

Answer 1

BDZ works on the GABA receptor specifically on A-receptor The GABA receptor has 2 Alpha, 2 BETA and one Y . It is found in the limbic system (this dictates the way someone behaves) When it form a ligland this stimulates the chloride channel to open to allow the passage of chloride ions resulting in hyper polarisation thus reducing the action potential of the neuron.. GABA receptor is an inhibitory receptor this mean it reduces the neurotransmission.

BDZ drugs can be long acting (1-3 days), intermediate-acting (10-20 hrs) or short-acting (3-8 hrs)

available IV,IM,oral, rectal

Question 2

What is the function of BDZ

Answer 2

reduce anxiety

Sedative and hypnotic actions (treat amnesia)

amnesia

muscle relaxant (for muscle disorder)

Anticonvulsant (for seizures)

Question 3

List BDZ drugs 
rule 
DE
or/and 
Pam

Answer 3

Chlordiazepoxide

Hidazepam

Nitrazepam

Diazepam

Question 4

Side effects of BDZ

Answer 4

Dependance, tolerance

Drowsiness and confusion

Precaution(alcoholics, liver disease, glaucoma, older people)

Question 5

BDZ Antagonist and medication

Answer 5

Flumazenil [floo-MAZ-eh-nill] is a GABA-receptor antagonist that can rapidly reverse the effects of benzodiazepines. The drug is available for intravenous (IV) administration only. Onset is rapid, but duration is short, with a half- life of about 1 hour. Frequent administration may be necessary to maintain reversal of a long-acting benzodiazepine. Administration of flumazenil may precipitate withdrawal in dependent patients or cause seizures if a benzo- diazepine is used to control seizure activity. Seizures may also result if the patient ingests tricyclic antidepressants (TCAs). Dizziness, nausea, vomiting, and agitation are the most common side effects.

Question 6

Explain the alternative Bendodiazepine

Answer 6

This drug is given short term for anxiety. buspirone displays some affinity for DA2 dopamine receptors and 5-HT2A serotonin receptors.

Contraindications= Epilepsy

Side effects= Abdominal pain, anger,, anxiety. chest pain, cold sweat, confusion, headache, dry mouth.

The frequency of adverse effects is low, with the most common effects being headaches, dizziness, nervousness, and light-headedness. Sedation and psychomotor and cognitive dysfunction are minimal, and dependence is unlikely. It does not potentiate the CNS depression of alcohol. Buspirone has the disadvantage of a slow onset of action. Figure 9.7 compares some of the common adverse effects of buspirone and the benzodiazepine alprazo- lam.

Zaleplon= Minimum withdrawal effects, no muscle relaxing effects

Question 7

What is the mechanism of Barbiturates

Answer 7

Barbiturates has a similar mechanism to BDZ however it combine on the opposite binding site to BDZ alpha and beta, but mainly alpha. Unlike BDZ, the chloride ion channel opens for a longer duration, additionally, after administration of the barbiturates it will still remain in the system and without the drug present it will still cause an affect.

Question 8

What are the main purpose of Barbiturates

Answer 8

Anxiety
sleep
sedation
seizures

Question 9

What are the side effect and precautions of taking barbiturates

Answer 9

respiratory depression

depression of CNS

small therapeutic index (drug dependance, tolerance and overdose)

drowsiness

tiredness

poisoning

Question 10

Other hypnotic drug

Answer 10

Zaleplon= similar to BDZ however quick in action due to the fact that the drug is eliminated from the system fast

Question 11

List drugs

Answer 11

Chlordiazepoxide
Nitazepam
Diazepam
Hidazepam

Other
valerian tincture (herb) sleep
Melatonin (Hormone)
Corvalol (herb)
Zopliclone
Zaleplon (sleep)
Buspirone (anxiety)