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Pharmacology 2 > Topic 8 - Neuroleptics (major tranquilizers) > Flashcards

Topic 8 - Neuroleptics (major tranquilizers) Flashcards

1
Q

What are neuroleptic drugs?

A

Known as antipsychotic medications, are medications that block dopamine receptors in the nervous system

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2
Q

Major groups of neuroleptic drugs

A

Phenothiazines
Butyophenones

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3
Q

Definition of phenothiazines

A

Used as tranquilizers, preanesthetic, antiemetic and as treatment fro CNS agitation after specific drug overdoses

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4
Q

Definition of butyophenones

A

It is more potent than phenothiazines. It has some analgesic (painkiller) effect

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5
Q

Active substances of phenothiazines

A

Acepromazine
Chlorpromazine
Propionylpromazine
Prometazine

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6
Q

Active substances of butyophenones

A

Azaperone (SU)
Dropeidol
Flunanisone
Haloperidol

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7
Q

Phenothiazine, mechanism of action:

A
  1. Dopaminergic receptor, antagonistic
  2. Alpha-adrenoreceptor antagonistic
  3. Muscarinic receptor
  4. Histamine receptor antagonistic
  5. Serotonin receptor antagonistic
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8
Q

Which effect does the dopaminergic receptor antagonistic have?

A

Antipsychotic effect, Antiemetic effect, Prolactin
increase, Parkinson-syndrome

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9
Q

Which effect does the Alpha-adrenoreceptor antagonistic have?

A

Hypotension, Sedation

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10
Q

Which effect does the Muscarinic receptor antagonistic have?

A

Mainly side effects

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11
Q

Which effect does the Histamine receptor antagonistic have?

A

Sedation, Antiemetic effect

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12
Q

Which effect does the Serotonin receptor antagonistic have?

A

Enhancement of several effects

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13
Q

Pharmacological effect of phenothiazone

A

Sedation (catalepsy like immobilization),
Potentiation (sedatives, hypnotics, analgesics),
Vegetative tone decrease, with increased relative
sympathetic tone, circulation, central antiemetic
effect, antihistamine activity, inhibition of
regulation of body temperature

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14
Q

Pharmacokinetical properties of phenothiazine

A

Absorption: Poor oral absorption (F=0.2): better in buccal, rectal use

Distribution: Good tissue distribution: cross BBB. Slow onset of activity (after IV use too), Long duration
of activity (>10-12 h) larger dose increase, plasma protein binding approx 95%

Metabolism: metabolism in liver

Excretion: excretion via urine, in metabolites, Slow
elimination from the body (Equidae 122/2013 EC
reg).

Long withdrawal period (Cascade)

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15
Q

Side effects of phenothiazine

A

1.TI (therapeutic index) relative big

2. Hypotension: collapse, in horses excitation

3.Tissue irritation, allergy, liver injury, hypothermia,
Penile Prolapse in horses and third eyelid (nictating membrane) prolapse in pets (cats, dogs), Prolactin increase, FSH, LH and oxytocin decrease. Epilepsy, extrapyrimidal symptoms (higher dose, tremors, shivering, ridgidity)

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16
Q

Indications for phenothiazine

A

'’1.** Calming, sedation of aggressive animals, eg. To
alleviate handling during veterinary investigations
and transport (without hypnotic effect: catalepsy like)

2. Premedication before general anaesthesia and
neuroleptanalgesia

17
Q

Contraindications for phenothiazines

A

1. May cause paradoxical reactions and phobias can get worse

2. Decreased motoric activity (without analgesia)

3. Not for dehydrated animals or in case of shock

4. Not for epileptic and pseudopregnant animals

5. Bulldogs and Boxers may be oversensitive: idiosyncracy, MDR 1 Gene Breeds (+/+)

6. Do NOT use before transportation to Abattoir
(slaughterhouse)

18
Q

Administration of phenothiazines

A

IV
IM
PO
(Buccal, rectal)

19
Q

Dosages for phenothiazones

A

Dosages in a large range (interspecies differences)

0.05 - 5 mg/kg

20
Q

Butyrophenones, mechanism of action

A

1. Dopamine Inhibition (D2)
2. NA (Noradrenaline) inhibition
3. Anticholinergic effects in CNS
4. With weaker antagonistic effect on alpha1 and H1 (histamine) receptors

21
Q

Butyrphenones, pharmacological effect

A

More potent than phenothiazines, some analgesic effect

22
Q

Side effects of butyphenones

A

Transient salivation or panting

Hypotension, respiratory stimulation, Boar penile
prolapse

23
Q

Contraindications for butyrphenones

A

Avoid use in very cold condition (but can reduce hyper thermia caused by Halothane)

Pharmacology 2 (9 decks)

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