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Pharmacology > Psychotropic substances > Flashcards

Psychotropic substances Flashcards

1
Q

Psychosedative effect

A

Depression of cortical function

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2
Q

Psychostimulation

A

Stimulation of cortical function

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3
Q

Cortical functions are found where - and involve what

A

Cerebral cortex: consciousness, memory, thought

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4
Q

Subcortical functions are found where, and involve what

A

Centres in subcortical regions: emotions, moods, experiences

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5
Q

What is meant by sedative effect

A

Suppression of all psychological processes (mental and motor activity)
1. Reaction speed and accuracy
2. Learning, memory and conditioned reflexes

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6
Q

Tranquilizing effect

A

Effect that suppresses negative emotions
(fear, anxiety, restlessness, sadness, anger)

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7
Q

Euphorizing effect

A

Facilitation of positive emotions, causing a sense of well-being

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8
Q

Antidepressant effect

A

Elimination of worsened mood, depression

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9
Q

Psychosis

A

Sensory and thought disorder, hallucinations, obsessive thoughts (delusions)

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10
Q

Neurosis

A

Neurotic disorder, irritability and other such effects resulting from psychological overload

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11
Q

What are neuroleptics and tranquilizers described as in veterinary medicine

A

Major tranquilizers

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12
Q

Neuroleptics do what

A

Depress the activity and dynamic of psychological processes, and act antipsychotically

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13
Q

Name some groups of neuroleptic drugs

A
  1. Phenothiazines
  2. Thioxanthenes
  3. Butyrophenones
  4. Indoles
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14
Q

Pharmacokinetics of neuroleptics

A
  • Good absorption - penetrate the BBB; metabolism in liver
  • Suppress all mediatory systems in brain and in periphery
    >Adreno, histaminergic, serotonin, cholino and
    dopaminoreactive systems
  • Main effect primarily related to dopaminergic transmission in CNs being blocked
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15
Q

What is the synthesis pathway of noradrenaline

A

Tyrosine
L-DOPA
Dopamine
Noradrenaline

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16
Q

Where does dopamine function in

A

Brain structures related to regulation of psychology:
- Striatum, Hypothalamus, Hippocampus, Mesolimbic structures and the 4th ventricle

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17
Q

Dopamine receptors

A

5 subtypes. Pharmacologically important are D1, D2 and D3

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18
Q

Effect of neuroleptics is realised through which receptors

A

Dopamine 2 receptors

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19
Q

Dopamine is broken down by what

A

MAO - monoamine oxidase
and COMT - Catechyl-o-methyltransferase

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20
Q

Manifestation of action of antipsychotic effect is linked to which receptors

A

Dopamine blocking effect
-> Limbic and cortical dopaminergic transmissions are blocked

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21
Q

Manifestation of action of sedative effect is linked to which receptors

A

Cholino and histamine blocking effect

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22
Q

Manifestation of action of hypothermic effect is linked to which receptor

A

Serotonin-blocking effect.
Linked to neuroleptic effect on the thermo-regulatory centre located in the hypothalamus

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23
Q

Manifestation of action of antiemetic effect is linked to which receptor

A

Dopamine blocking effect.
Strong in humans, dogs and monkeys - weak in cats.
NL suppress vomiting of different genesis

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24
Q

What are some cardiovascular effects of Neuroleptics

A

Blockade of central and peripheral effects of catecholamines
1. Alfa-blockade - peripheral vasodilation
2. Arterial hypotension- up to shock like conditions
3. Hypotensive effects in anesthesised, debilitated or
hypovolemic patients esps.
4. Phenothiazine can potentiate arterial hypotensive effects
of local anesthetics in case of regional anesthesia

25
Q

What are some respiratory effects of neuroleptics

A

Clinical doses have little effect
Respiratory rate often depressed - minute volume remains normal.
Respiratory depression may be exaggerated when phenotiazines administered with other CNS respiratory depressants (opioids, isoflurane) or in high doses

26
Q

Musculoskeletal effects of Neuroleptics

A

Phenotiazines provide good muscle relaxation
- Often used in conjunction with anesthetics that do not provide muscle relaxation or that result in muscle rigidity (ketamine)

27
Q

How do phenotiazines alter thermoregulation?

A

By decreased catecholamine binding in hypothalamus
+ Altering vasomotor tone in peripheral vessels that participate in heat retention and elimination

28
Q

Effect of phenotiazines on blood

A

Markedly reduces hematocrit in animals

29
Q

Interactions of neuroleptics with other medicinal products

A
  1. Increase potency of hypnotics (don’t cause sleepiness by
    themselves)
  2. Make effect of general anesthetics more potent
  3. Increase potency of analgesics without having any analgesic effect by themselves
  4. Potenciate muscle relaxation effect
  5. Use in caution with drugs that also produce vasodilation
    or hypotension
30
Q

Contraindications of neuroleptics

A

Phenotiazines should not be used in patients that are dehydrated, hypovolemic, bleeding or in shock (vasodilation)
- Don’t use in patients with coagulopathies or trombocytopenia
- Use cautiously in brachycephalic dogs and debilitated animals

31
Q

Classification of tranquilizer drugs

A
  1. Ataractic drugs or muscle relaxant sedative tranquilizers
    -Diazepam, Midazolam, Lorazepam
  2. Vegetosedative tranquilizers
    • Amisyl
  3. Sedative tranquilizers
    • Valerian
    • Bromine salts
32
Q

Pharmacokinetics of Tranquilizers

A

Administer through oral and parenteral route
Absorb well, penetrate BBB and placental barrier
Metabolised in liver - occurence of enzyme induction
Half-life in animals - couple hours but accumulation frequent

33
Q

Mechanism of action of tranquilizers

A

Effect through benzodiazepine receptors, gamma-aminobutyric acid (GABA) receptors and barbiturate receptors
->Impact the chloride ionophore complex

34
Q

Usage of tranquilizers

A

Diazepam: no 1 against convulsions
Premedication before anesthesia
Tranquilizing animals
Relaxation of skeletal muscles
In case of joining “unfamiliar” animals

35
Q

CNS effects of tranquilizers

A

Benzodiasepines cause reduction in cerebral blood flow
In healthy patient, behavioral effects mild. In young, old and sick animals - sedation more reliable

36
Q

Cardiovascular effects of tranquilizers

A

Clinical dose causes minimal depression
High doses: reduction in mean arterial blood pressure & systemic vascular resistance and reduction in myocardial oxygen consumption

37
Q

Musculoskeletal effects of tranquilizers

A

Benzodiazepines potentiate the GABA-ergic-mediated musccle relaxation - anticonvulsant effect

38
Q

Adverse effects of tranquilizers

A

Transient period of agitation, vocalisation, excitement, muscle fasciculations and ataxia
esps. in dog, cat and horse.

39
Q

Contraindications of tranquilizers

A

Patients with hypersensitivity to benzodiazepines and with hepatic dysfunction

40
Q

Benzodiazepine antagonist

A

Flumazenil
>Competitively antagonises the action of BA on the receptor

41
Q

a2 adrenomimetics

A

Act in adrenergic synapses
Used in combination with sedatives or neuroleptanalgesia drugs
Only used as sedatives in veterinary medicine

42
Q

Xylazine effects

A

Analgesic, sedative, muscle relaxant

43
Q

Pharmacokinetics of a2 agonists

A

Administered through injection
Metabolism is quick - many metabolites are created
half-life depends on species of animal and particular drug

44
Q

Pharmacodynamics of a2 agonists

A

Centralised effect.
Stimulates a2 adrenergic receptors.
Inhibits release of noradrenaline in adrenergic synapse

45
Q

CNS effects of a2 agonists

A

Reliable sedation by activation of a2 receptors in locus coeruleus nucleus in brainstem
activation will cause agitation, increased locomotor activity. Animal may show paradoxical excitement or movement

46
Q

Analgesia of a2 agonists

A

Similar to those of morphine, but unlike morphine, does not cause CNS stimulation, but rather sedation and depression

47
Q

Gi effects of a2 agonists

A

Inhibit of impulses is accompanied by activation of the vomiting centre - dogs and cats often experience vomiting as a side effect
Cannot be inhibited using a-adrenoblockers
GI motility and acid secretion is reduced

48
Q

Cardiovascular effects of a2 agonists

A

Biphasic response
Initial phase: activation of central a2 receptors reduce sympathetic outlofw -> parasympathetic tone increase
-> Negative inotropic, chronotropic and dromotropic effect on heart

Peripherally a1 and a2 receptors are activated in blood vessels. Increase in arterial blood pressure -> baroreceptor mediated reflex bradycardia follows.
Patients hypertensive and bradycardic.
Then bp decreases, patients hypotensive and bradycardic.

49
Q

Respiratory effects of a2 agonists

A

Generally cause a centrally mediated reduction in respiratory rate and minute ventilation

50
Q

Reproductive effects of a2 agonists

A

In pregnant animals, low doses can decrease myometrial contractions of uterus - high doses increase them.
In non-gravid uterus, myometrial contractions can be observed at any dose of a2 agonists

51
Q

Species specificity of a2 agonists

A

Ruminants are the most sensitive - cattle’s dosage is 1/10 of horse’s!
Ineffective in pigs - doses are large

52
Q

Contraindications of a2 agonists

A

Don’t administer in combination with adrenaline - xylazine makes heart extremely sensitive to effect of it.
Not with tendency for arrhythmia, hypotension, shock, renal impairment, liver impairment or epilepsy (it predisposes cramping)
Not in last month of gestation -> abortion / premature birth

53
Q

Name 2 antidepressant drug types

A

Fluoxetine and Clomipramine

54
Q

Indication of antidepressants

A

To dogs in event of separation anxiety related disorders that result in irritation, unintentional defacation and urination

55
Q

Fluoxetine

A

Selective serotonin reuptake inhibitor
No sedative effect
Must not be administered together with products that increase risk of abnormal muscle contractions (phenothiazines), other serotonergic substances and monoamine oxidase inhibitors, tricyclic amines

56
Q

Clomipramine

A

Non-selective serotonin reuptake inhibitor
Anticholinergic effect through the antagonism of muscarinic receptors

57
Q

Mirtazapine

A

For bodyweight gain of cats experiencing poor appetite and weight loss resulting from chronic medical conditions
a-2 adrenergic receptor antagonist; noradrenergic and serotonergic antidepressant drug.

58
Q
A

Pharmacology (18 decks)

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