Tranquilliser sedatives

Question 1

Phenothiazines

Answer 1

1 - Chlorpromazine

2 - Propionylpromazine

3 - Azepromazine

4 - Thiethylperazine

5 - Promethazine

Question 2

Butyrophenones

Answer 2

1 - Azaperone

2 - Droperidol

3 - Fluanisone

Question 3

Pharmacological effects of tranquilliser sedatives.

4

Answer 3

1) Decreased motor activity
2) Decreased aggression
3) No analgesic activity, but they potentiate the activity of analgesics (neuroleptanalgesia). Slight analgesic activity can be observed by butyrophenones.
4) Increased dose = increased duration of sedation, not depth. (Do not cause hypnosis).

Question 4

Receptorial effects of tranquilliser sedatives.

5

Answer 4

ANTAGONIST OF:

alpha 1 –> Vasodilation, hypotension. (Do NOT use in dehydrated patients, first IV fluid. Boxers sensitive.)

Dopamine –> sedation, antiemetic, convulsions, pseudopregnancy.

Histamine –> anti-allergy.

Serotonin –> sedation, disturbed thermoregulatory center.

Ach-m –> very mild PS-lytic, dry mouth, constipation (esp. humans)

Question 5

Indication/use of tranquilliser sedatives

4

Answer 5

• Sedation (e.g. transportation, capturing)
• Antiemetic
• Premedication
• Neuroleptanalgesia

Question 6

Side effects of tranquilliser sedatives.

10

Answer 6

1) Hypotension –> shock –> death (dehydration: boxer)
2) Horse, paradox rxn: feel hypotension –> release adrenaline –> excitation
3) Horse penis prolapse
4) Convulsions (not for use in epileptic patients)
5) Pseudopregnancy
6) Disturbed thermoregulation
7) SC & IM: pain due to tissue irritation
8) Low PO bioavailability
9) Very long half-life –> long WP
10) Decreased FSH-secretion: fertility rate decreases

Question 7

Chlorpromazine

Answer 7

Paradox rxn: muscle necrosis
- very slow excretion from the body

A.U.V.: -
Human:

Question 8

Acepromazine

Answer 8

Most used.

A.U.V. - Licensed for dogs + horses. All administrations, but IV preferred.
(ACP inj., tablet, Vetranquil inj., Sedalin oral gel.)
Human: -

Question 9

Thiethylperazine

Answer 9

Pronounced antiemetic activity.

A.U.V.: -
Human: (Tercan inj., dragee, suppository)

Question 10

Promethazine

Answer 10

Pronounced antihistamine activity.

A.U.V.: -
Human: (Phenergan (Pipolphen) tablets, inj., suppositories)

Question 11

Pharmacological effects of butyrophenones.

3

Answer 11

1) Slight analgesic activity
2) Compensation of the respiratory depressand effect of opiates –> excellent for neuroleptanalgesia.
3) Less cardiovascular depression and inhibition of temperature center.

Question 12

Azaperone

Answer 12

For sedation of pigs, reducing stress.

A.U.V.: Licensed for swine. Only IM injection bc IV causes hypotension. (Stresnil inj.)
Human: -

Question 13

Droperidol

Answer 13

Rodent + lab animal surgery w/ fentanyl (neuroleptanalgesia)

A.U.V.: -
Human: Inapsine inj.

Question 14

Fluanisone

Answer 14

Rodent + lab animal surgery w/ fentanyl (neuroleptanalgesia)

A.U.V.: Hypnorm inj.
Human: -