Topic 9 - Sedato-Hyponotics Flashcards

1
Q

Name the groups of sedato-Hyponotics

A

1. Alpha 2 agonists
2. Alpha 2 antagonists
3. Barbiturates
4. Benzodiazepines

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2
Q

Active substances of Alpha 2 agonists

A

Xylazine
Medetomidine
Dexemedetomidine
Romifidine
Detomidine

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3
Q

Active substances of Alpha 2 antagonists

A

Atipamezole
Yohimbine
Telazoline

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4
Q

Active substances of Barbiturates

A

Long Acting:
Barbital
Phenobarbital

Middle long acting
Amobarbital
Butobarbital

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5
Q

Active substances of Benzodiazepines

A

Diazepam
Alprazolam
Lorazepam
Zolazepam
Midazolam

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6
Q

Mechanism of action for alpha 2 agonists

A

1.Postsynaptic alpha 2 ⭢ Alpha 1 activation
2. Presynaptic alpha 2 activation

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7
Q

Effects of Postsynaptic alpha 2 ⭢ Alpha 1 activation

A

vasoconstriction, transient hypertension, reflex bradycardia hypotension

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8
Q

Effects of Presynaptic alpha 2 activation

A

sedation, analgesia (short term)
Decreased motor activity recumbency
+ GNG hyperglycemia
GIT relaxation : bloat, tympani

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9
Q

Alpha 2 agonists pharmacokinetics: Xylazine

A

A: Fast
D: Good
M: liver (2-amino metabolite)
E: with urine

Transport: bounded to plasma proteins

Onset of sedative effect: IV few min. IM 10-15min

Duration of sedation: 0.5-1 hour

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10
Q

Alpha 2 agonists pharmacokinetics: Detemodine

A

A: Fast
D: Good
M: Liver
E: with urine

Transport: bounded to plasma proteins

Onset of sedative effect: IV immediately, IM few min

Duration of sedation: 1-6 hours

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11
Q

Alpha 2 agonists pharmacokinetics: Medetomidine

A

A: fast
D: good
M: liver (hydroxyl met)
E: with urine

Transport: bounded to plasma proteins (85%)

Onset of sedative effect: IV immediately, IM few min

Duration of sedation: 0.75 - 1.5 hour

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12
Q
A
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13
Q

Side effects of Xylazine?

A

Emesis and vomiting in cats and dogs.
Bradycardia, malignant arrhythmias, sweating in
horses, ecbolic action: in late pregnancy its use is contradicated. Tympani in ruminants

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14
Q

Side effects of Detomidine

A

Hyper tension, then hypotension, bradycardia, respirstory depression, diuresis (micturition),
hypothermia,sweating, snoring, tremor

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15
Q

Indications of xylazine

A

Sedative-analgesic drug with depressed motor activity can be used in all domestic animals
(swine low potency). Analgesic effect is short (10-15 min.).

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16
Q

Indications of Detomidine

A

More potent drug than xylazine, licensed for equine use. Does not cause total loss of consciousness (at therapeutic dose). Duration of
action is application route and dose dependent.

Use: alone or in combination with ketamine, thiopentone, opioids

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17
Q

Indications of Medetomidine and Dexmedetomidine

A

Effects are similar to those o f xylazine but it seems to be more reliable and safer.

  • Developed for cats and dogs. Duration of action is dose dependent. Sedation 1-3 hours (DM 2 hours). Analgesia 5-15 min., however DM 90 min.
18
Q

Indications of Romifidine

A

(Frequently in combination with Buthorphanol (20 μg/kg)).

Duration: Sedation a bit longer and causes less ataxia or recumbency than Xylazine
and Detomidine.

19
Q

Pharmacological effect of alpha 2 Agonists

A

1. Activation of Postsynaptic (peripheral)
2. Activation of Presynaptic (Central)
3. Sedative
4. Analgesic
5. Reduced motor activity

20
Q

Antidotes of alpha 2 agonists

A

Atipamezole, Tolazoline, Yohimbine

reverses the effect of alpha 2 agonists

21
Q

Dosage of xylazine

A

horse: 2-3 mg/kg IM, 0.5-1.0 mg/kg IV
cattle: 0.05-0.2 mg/kg IM
dog:1-2 mg/kg IM
cat: 3 mg/kg IM (emesis induction 0.5-1 IV).

Growth hormone stimulation
test (100 μg/kg b.w. IV)

22
Q

Dosages of detmodine

A

10-80 μg/kg IM or IV

40 μg/kg PO

23
Q

Dosage of Medetomidine

A

Dogs: 10-80 μg/kg (alone) IM
or IV 10-20 μg/kg (combination)

cats: 50-150 μg/kg IM

24
Q

Dosage of Dexmedetomidine

A

dogs & cats: 375 μg/m2 IV, 500 IM μg/m2* (cats only IM) premedication 125-375 μg/m2
Dog 125 μg/m2 PO

25
Q

Dosage of Romifidine

A

Horse, dog: 40-120 μg/kg IV, IM
Cat: 200-400 μg/kg IV, IM

(Frequently in combination with Buthorphanol (20 μg/kg))

26
Q

Mechanism of action of Alpha 2 Antagonist

A

Atipamezole: Alpha 2 adenoreceptor blocking agent. Reverses the effect of medetomidine (and other alpha 2 agonists)

Yohimbine and Telazoline: much less specific alpha 2 adenoreceptor antagonists than
atipamezole, and so have significant alpha 1 antagonistic action. Reverses the effect of
Xylazine

27
Q

Side effects of Alpha 2 Antagonist

A

Well tolerated by dogs and cats.

tachycardia (high dose), transient hypotension, hypothermia,
vomiting, defecation, panting, muscle tremor

28
Q

Contraindications of Alpha 2 Antagonist

A

Ketamin-medetomidine (horse, dog)

29
Q

Dosage of Alpha 2 Antagonist

A

Atipamezole:
horse: 150 μg/kg,
dogs: 5 times he dose of medetomidin
cats: 2.5 times the dose of medetomidin

30
Q

Mechanism of action of Barbiturates

A

Decrease in Ca2+ accumulation
→ inhibition in release of stimulatory transmitters, stabilisation of presynaptic
membranes.

General inhibition of CNS, but sensitivity of certain structures differs (paradox phenomenon,
some are suitable for general anaesthesia)

31
Q

Pharmacological effect of barbiturates

A

CNS, circulation, respiration – inhibition (last two only in case of overdosing), sedative, hypnotic and mild anxiolytic effect,
significant anticonvulsant effect*

32
Q

Side effects of barbiturates

A

Ataxias, over sedation, longer use CYP450 induction, liver toxicity, PU/PD, polyphagia, obesities

33
Q

Dosage of barbiturates

A

Dogs, cats: PO 1.5-5 mg/kg B.I.D.
Tetanic horses: IV 12 mg/kg initial, 6 mg/kg B.I.D. to maintain

34
Q

Mechanism of action of benzodiazepines

A

Facilitate or amplify the inhibitory activity of GABA, possibly by eliciting a structural alteration
in the GABA-receptor complex, which results in the opening of chloride ion channels. (Positive
Allosteric Activators). BZD-receptors are located in all levels of CNS (and in muscles).

Open GABA-gated Cl- ion channels CNS, muscle
depression

Bind at BZD site open GABA-gated Cl- channel: hyperpolarization

35
Q

Pharmacological effect of benzodiazepines

A

Sedation and anxiolytic effect
Anticonvulsive effect
Muscle relaxation
Hypnotic

In animals: they are primarily sedatives, but they
also have a hypnotic effect with increasing dose. They can be combined with other agents;
sedatives, hypnotics, and anaesthetics. Sedation
of patients requiring intensive care and/or in high risk patients (e.g. patients at cardiovascular risk).

Sedation and pre-anesthetization of animals, safely even in very young animals (e.g. young
foals) and in the elderly - Epileptic seizure.

Decreases possibility of seizures caused by other drugs. Before myelography.

36
Q

Pharmacokinetics of benzodiazepines

A

Diazepam:
A: Oral absorption is good. IM delayed

Significant binding to plasma proteins (interactions)

E: after demethylation and conjugation via the kidney (first metabolite is active: entero-hepatic recirculation, liver disease may prolong activity,
interactions)

37
Q

Indications of benzodiazepines

A

Diazepam:
1. Premedication and combination (ketamine)

2.Muscle relaxation

3. Prevention and control of epilepsy

4. Sedation (taming during grouping of animals)

38
Q

Contraindications of Benzodiazepines

A

Diazepam
- Paradoxical reaction in Cat, Greyhound
- Inhibition of respiration (aminoglycosides increase)
- Before and during deliver y (high doses are contraindicated)
- Liver diseases (rare hepatotoxicity mainly in cats
and foals)

39
Q

Antidotes of Benzodiazepines

A

In case of overdoses!

Flumazenil (F)
Sarmazenil (S)

40
Q

Dosages of Benzodiazepines

A

100 (F) μg/ttkg or 40 (S) μg/ttkg (horses) IVq24h

Diazepam:
sedation: 1-1.5 mg/kg PO
pre-medication: 0.2 mg/kg IV
status epilepticus: 5-10 mg/dog IV or rectally
(if needed then 2-5 mg/hour IV glucose inf.)
Cats 2-3 mg IV induction of prot feed intake

Midazolam:
Horses: 0.05-0.2 mg/kg IV
Dogs, Cats: 0.1-0.5 mg/kg IV, 0.3-1 IM