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Pharmacology I > 11. CNS stimulant. Anticonvulsant drugs > Flashcards

11. CNS stimulant. Anticonvulsant drugs Flashcards

1
Q

Seizures are caused by…

A
  • Abnormal, high-frequency discharge of a group of neurons
  • Starting locally → Other parts of the brain
  • Progressive
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2
Q

Seizures affect which nervous phenomena?

A
  • Motility
  • Sensation
  • Behaviour
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3
Q

During a seizure, unconsciousness occurs when…

A

The reticular formation (group of nuclei) is involved

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4
Q

Seizures are preferred to be treated by…

A

Monotherapy

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5
Q

Combination therapy during seizures involves…

A

Any 2 of:

  • Phenytoin
  • Phenobarbital
  • Carbamazepine
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6
Q

Drug treatment of: Status epilepticus

A

Diazepam

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7
Q

Drug treatment of: Seizures

A
  • Phenobarbital
  • Phenytoin
  • Valproic acid
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8
Q

Phenobarbital: Summary

A

Safe, effective & inexpensive barbiturate for chronic therapy in dogs & cats

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9
Q

Phenobarbital: Mechanism of action

A
  1. ↑ Activity of GABA (Inhibitory neurotransmitter)
  2. Opens Cl- channels in excitatory cells
  3. Neuronal inhibition
  4. ↓ Neuronal excitotoxicity (via glutamate receptors)
  5. Inhibition of voltage-gated Ca2+ channels
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10
Q

Phenobarbital: Pharmacokinetics

A
  • Rapidly absorbed after PO
  • High bioavailability
  • Metabolised primarily in the liver
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11
Q

Phenobarbital: Side effects

A
  • Sedation
  • Drowsiness
  • Ataxia (loss of body movements)
  • Polyphagia
  • Polyuria
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12
Q

List the benzodiazepines

A
  • Diazepam
  • Carbamazepine
  • Midazolam
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13
Q

Diazepam: Clinical uses

A
  • Status epilepticus: Preferred drug
  • Premedication & combination (ketamine)
  • Muscle relaxation
  • Prevention and control of epilepsy
  • Sedation
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14
Q

Diazepam: Administration

A
  • Rectal
  • IV

Not suitable for PO

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15
Q

Carbamazepine

A

Similar profile as phenytoin but with fewer unwanted side effects

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16
Q

Phenytoin

A

Membrane stabilising agent

  • Short elimination half-life in dog
  • Extremely long in cat (toxicity)
17
Q

Midazolam

A
  • Shorter effect than diazepam
  • Produces less sedation than diazepam
18
Q

Drugs contraindicated in epileptic patients

A
  • Phenothiazine derivatives:
    • Propiopromazine
    • Acepromazine
    • Chloropromazine
  • Butyrophenones:
    • Azaperone
19
Q

CNS stimulants (analeptics) can be categorised into…

A
  • Convulsants & respiratory stimulants
  • Psychomotor stimulants
  • Psychotomimetic (hallucinogenic) drugs
20
Q

Convulsants & respiratory stimulants

A
  • Little clinical use → Used in experiments
  • Doxapram = Respiratory stimulant in acute resp. failure
  • Strychnine, PTZ = Induce convulsions
    • PTZ (tests antiepileptic drugs)
21
Q

Psychomotor stimulants

A
  • Amphetamines
  • Cocaine
22
Q

Amphetamines

A
  • ↑ Motor activity
  • Euphoria-excitement
  • Anorexia
  • Psychotic behaviour after prolonged use

Due to release of catecholamines

Effect for a few hours, followed by depression/anxiety

23
Q

Amphetamines: Clinical use

A
  • Narcolepsy
  • Hyperkinetic children
24
Q

Cocaine

A
  • Inhibition of catecholamine uptake (esp. dopmine) by nerve terminals
  • Shorter duration
  • Similar to amphetamines
  • Main importance: Abuse
25
Q

Methylxanthines: Examples

A
  • Caffeine
  • Theophylline (bronchodilator)
26
Q

Methylxanthines: Effect

A
  • ↓ Fatigue
  • ↑ Mental performance without euphoria
  • CNS stimulation
  • Diuresis
  • Stimulation of cardiac muscle
  • Relaxation of bronchial muscles
27
Q

Psychotomimetic drugs: Examples

A
  • LSD
  • Mescaline
  • MDMA
  • Phencyclidine
28
Q

Psychotomimetic drugs: Effects

A
  • Affects thoughts and mood without psychomotor stimulation
  • Some can cause acute hyperthermia and death
  • 2 main groups
    • Drugs acting on 5-Hydroxytryptamine
    • Catecholamines
29
Q

Effect of LSD, Mescaline and MDMA

A
  • Ecstacy: Inhib 5-HT uptake
  • MDMA also affects many other receptors
    • Psychomimetic effect
    • Stimulant effect
  • Can cause acute hyperthermia and death
30
Q

Phencyclidine: Mechanism of action

A

Blocks glutamate activated NMDA receptors

31
Q

Barbiturates: Mechanism of action

A

GABA-BDZ-Barbiturate-Receptor Complex (GABAA)

  • ↓ Ca2+ accumulation → inhibition of stimulatory transmitter release → Stimulation of membranes
32
Q

Barbiturates: Effects (general)

A
  • CNS effect
  • Circulatory effect
  • Respiratory effect

Pharmacology I (19 decks)

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