Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharma 1 > Tranquillisers and sedatohypnotics > Flashcards

Tranquillisers and sedatohypnotics Flashcards

1
Q

Some small-molecule neurotransmitters:

A

Exitatory:

  • acetylcholine
  • norepinephrine
  • dopamine
  • Glutamate and Aspartate
  • 5-Hydroxytryptamine, Serotonin
  • Histamine

Inhibitory:

  • acetylcholine
  • norepinephrine
  • dopamine
  • Glycine
  • GABA
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Classification of CNS stimulants

based on their site of action:

A 
Cortical:
– xanthines (coffeine, teophylline, theobromine)
– cocaine
– ephedrine, amphetamines
– Psychotomimetics (e.g. LSD)
• Medullar:
– xanthines (coffeine, teophylline, theobromine)
– pentetrazole
– doxapram
– picrotoxin

• Spinal:
– strychnine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Doxapram

A

Short-acting respiratory stimulan

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Convulsants and respiratory stimulants

analeptics

A
  • Doxapram
  • Picrotoxin
  • strychnine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Psychotomimetic drugs

hallucinogens

A
  • LSD
  • MDMA
  • Mescaline
  • Psilocybin
  • Phencyclidine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Psychomotor stimulants

A

Amphetamine and related compounds:

e. g.dexamphetamine
- methylamphetamine
- methylphenidate
- fenfluramine

  • Cocaine
  • Methylxanthines, (e.g. caffeine,
    theophylline)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

CAFFEINE

four identifiable actions in vitro

A
  1. Adenosine receptor blockade. (primarily)
    = nonselective antagonist
  2. Phosphodiesterase inhibition
  3. Action at Ca++ channels to increase entry of Ca++ into
    cells
  4. Binding to GABA receptors at the benzodiazepine
    site and decrease release

at high dosages may be associated with positiveinotropic and chronotropic effects on the heart + elevation of blood pressure.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Which drug can neutralize the effects of benzodiazepine tranquilizers?

A

Caffeine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Certain short-acting respiratory stimulant that can be used in acute respiratory failure

A

e.g. doxapram

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

a convulsant poison that acts mainly on the spinal cord by blocking receptors for the inhibitory transmitter
glycine.

A

Strychnine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

acts as GABAA antagonists and appears to

block the ion channel:

A

Picrotoxin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

A. TRANQUILLISERS /“Major”/:

A

A. TRANQUILLISERS /“Major”/

  1. PHENOTHIAZINE DERIVATIVES
    - PROPIOPROMAZINE (Combelen)
    - ACEPROMAZINE (Vetranquil, Atrovet)
    - CHLORPROMAZINE (Hibernal)
    - PROMETAZINE (Pipolphen)
  2. BUTYROPHENONES
    -AZAPERONE (Stresnil)
    -(HALOPERIDOL, DROPERIDOL,
    FLUANISONE)
  3. (RAUWOLFIA ALKALOIDS - reserpine)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

B. HYPNOSEDATIVES (SEDATIVE-HYPNOTICS)

4 groups and their drugs:

A
  1. ALPHA2-AGONIST
    - XYLAZINE
    - MEDETOMIDINE, DEXMEDETOMIDINE
    - ROMIFIDINE
    - DETOMIDINE
    ANXIOLYTICS (Minor tranquillisers)
  2. BENZODIAZEPINES
    - DIAZEPAM
    - CHLORDIAZEPOXIDE
  3. PROPANDIOL-DERIVATIVES
    - MEPROBAMATE
  4. OTHER compounds
    - BARBITURATES (long acting)
    - Alcohols, Aldehydes, Br–and Mg2+-salts
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

TRANQUILLISERS

Uses of Phenothiazines:

A
  • Calming, sedation
  • Muscle relaxation
  • Premedication
  • All drugs in this group have similar efficacy,
    they vary in potency and side effects
  • Slow onsets
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Side effects-contraindication of Phenothiazines:

A
  • Hypotention —> collapse
  • Tissue irritation, allergy
  • Penile prolapse (horses) and third eyelid
  • Epilepsy, Extrapyramidal symptoms (high dose)
  • not use before transportation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

TRANQUILLISERS

Phenothiazine derivatives:

A
  • CHLORPROMAZINE
  • PROPIOPROMAZINE
  • ACEPROMAZINE
  • PROMETAZINE
  • Perphenazine, Thiethylperazine, Fluphenazine, Trifluoperazine
17
Q

CHLORPROMAZINE:

A

side effects -frequently
paradox reaction in horses (cyclic ataxic reaction with
excitation
- hypotension and tachycardia, rarely in other
animals), tissue irritation, allergy

18
Q

PROPIOPROMAZINE

A

PROPIOPROMAZINE

more reliable, less side effects

19
Q

ACEPROMAZINE

A

ACEPROMAZINE
more efficacious than chlorpromazine, less side effects
good oral bioavailability, Halothan hyperthermia and
arrhythmogenicity↓

20
Q

PROMETAZINE

A

PROMETAZINE
less potent tranquillizer, increased antihistaminic
and anti-5-HT effect

21
Q

Butirophenones

  • potency:
  • drugs:
  • in combination with:
  • side effects:
A

More potent than phenothiazines (some analgesic effect)
- In CNS dopamine-inhibition (D2),
NA-inhibition
anticholinergic effect
(with weaker antagonistic effect on α1-, H1-receptors)

Droperidol
Haloperidol
Fluanisone
AZAPERONE (only in Swine)

In combination with Metomidate.

Side effects-contraindication:
- transient salivation or panting,
- hypotension, respiratory stim., boar penile prolaps
- avoid use in very cold condition
(but can reduce hyperthermia caused by Halothane)

22
Q

The Most characteristic effects of

SEDATIVE-HYPNOTICS

A 
• Sedative effect
• Anxyolytic effect
• Hypnotic effect
- Hypnotic effect – drugs induce sleep
- Hypnogen drugs – to maintain sleep
• Muscle relaxation
• Anticonvulsive (exception alpha2-agonist)

These effects are dose dependent and the
efficacy of individual agents is different.

23
Q

ALPHA2-AGONISTS

Effects:

A 
ALPHA2-AGONISTS
• Sedative: locus coeruleus
• Analgesic: spinal cord
• Reduced motor activity: spinal cord
• Further effects:
- relaxation of GI smooth muscle
- mydriasis
- bulbar tension ↓
- ACTH secretion ↑
- insulin, renin, ADH ↓
- hyperglycaemia
- microsomal enzymes ↓
24
Q

Side effects of alpha2- agonists:

A
  • bradycardia
  • vasoconstriction
  • Hyoptension
  • Hyperglycaemia
  • AV block
  • hypopnoe
  • polyuria
  • emesis
  • tympanism
25
Q

XYLAZINE

  • effect
  • side effect
A

Sedative-analgesic drug with depressed motor
activity can be used in all domestic animals.
Side effects:
– emesis and vomiting in cats and dogs
– bradycardia, malignant arrhythmias
– sweating in horses
– ecbolicaction: in late pregnancy its use is
contraindicated
– tympani in ruminants

26
Q

DETOMIDINE

  • characteristics
  • side effects
  • combinations?
A

More potent than xylazine, licensed for equine use
Does not cause loss of consciousness
Duration of action is dose dependent
Side effects:
- hypertension, then hypotension
- bradycardia, respiratory depression, diuresis
- hypothermia, sweating, snoring, tremor
Use: alone or in combination with ketamine,
thiopentone, opioid drugs

27
Q

MEDETOMIDINE (M) DEXMEDETOMIDINE (DM)

  • effect
  • used in?
A
  • Effects are similar to those of xylazine
    but it seems to be more reliable and safer.
  • Developed for cats and dogs.
  • Duration of action is dose dependent.
28
Q

ALPHA2-ANTAGONISTS

  • Drugs
  • side effects
A

ATIPAMEZOLE:
Alpha2-adenoreceptor blocking agent.
Reverse the effect of medetomidine and other alfa2-agonists too
SIDE-EFFECTS: well tolerated by dogs and cats
tachycardia (high dose) transient hypotension, hypothermia, vomiting, defecation, panting, muscle tremor.
Contraindication: ketamin-medetomidine

YOHIMBINE and TELAZOLINE:
Much less specific alpha2-adenoreceptor antagonist than atipamezole, and so has significant alpha1-antagonistic action. Reverse the effect of xylazine.
Yohimbine is mainly used in conjunction with FAMPIRIDINE which facilitate the release of neurotransmitters form nerve
endings.

29
Q

BENZODIAZEPINES

  • receptor action
  • location
  • effects:
A
  • Receptoral action: they facilitate or amplify the inhibitory
    activity of GABA (Positive Allosteric Modulators)
  • BZD-receptors are located in all levels of CNS
    (and in muscle).
  • Effects: sedation and anxiolytic effect anticonvulsive effect, muscle relaxation, hypnotic
30
Q

Benzodiazepine antidote:

A

Flumazenil and Sarmazenil

31
Q

DIAZEPAM

  • administration
  • clinical use
A 
DIAZEPAM
Oral absorption is good. IM delayed.
Significant binding to plasma proteins.
• Clinical uses
- Premedication and combination (ketamine)
- Muscle relaxation
- Prevention and control of epilepsy
- Sedation (taming during grouping of animals)
32
Q

Midazolam

A

MIDAZOLAM

Shorter effect, produces less sedation than diazepam

33
Q

Anxiolytic drugs:

3 most NB

A
  • diazepam
  • midazolam
  • zolezepam
34
Q

BARBITURATES

  • effects
  • classification
A

Effects:

  • decrease in Ca2+ accumulation
  • stabilisation of membranes
  • CNS, circulation, respiration

Classification according to the duration of action:
long acting e.g. Barbital, Phenobarbital,
middle-long acting e.g. Amobarbital, Butobarbital

35
Q

SIDE-EFFECTS OF ALFA2-ADRENOCEPTOR:

A 
”AV” BLOCK 
BRADYCARDIA 
VASOCONSTRICTION 
HYPOTENSION 
HYPERGLYCEMIA 
HYPOPNOE 
POLYURIA
EMESIS (dogs, cats)
TYMPANISM (cattle)

Pharma 1 (15 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions