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D -rugs baby ;) Flashcards

1
Q

Why should hypnotics be reserved for short courses?

A

Because dependence and tolerance may occur with long term use - 4 weeks max use

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2
Q

Indications for hypnotics

A

To alleviate acute conditions after causal factors have been established e.g. short term insomnia due to shift work / emotional prob / serious medical illness

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3
Q

Most commonly used hypnotics

A

benzodiazepines

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4
Q

Mechanism of action for benzodiazepines (hypnotics)?

A

Benzodiazepines bind to receptor sites that are closely linked to the GABA-A receptor, inducing a conformational change that enhances the action of the inhibitory neurotransmitter GABA

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5
Q

What binds to the same receptor as benzodiazepines but isn’t a benzodiazepine?

A

Zopiclone

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6
Q

Examples of hypnotics

A

Tamezepam - oral at bedtime

Zopiclone - oral at bedtime

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7
Q

SE’s hypnotics

A

Drowsiness
Lightheadedness
Confusion
Ataxia (the loss of full control of bodily movements)
May impair driving next day
Paradoxical increase in anxiety and aggression; adjustment of the dose up or down usually improves the problem
Tolerance may develop within 3-14d

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8
Q

Cautions/ contraindications hypnotics and anxiolytics

A

Contraindicated in: resp depression, acute breathlessness, severe liver disease, myasthenia gravis, sleep apnoea syndrome

Withdrawal symptoms if drug stopped abruptly: anxiety, insomnia, depression, psychosis and convulsions

Elderly pts particularly sensitive - AVOID

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9
Q

Why should anxiolytics be reserved for short courses?

A

As with hypnotics, there is danger of dependence and tolerance following long term use

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10
Q

Anxiolytics indications for use

A

Short term relief in severe anxiety
In panic disorders resistant to antidepressant treatment
IV for short term sedation with medical procedures e.g. colonoscopy
Prevention of the alcohol withdrawal syndrome
Benzodiazepines also used in the acute management of status epilepticus

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11
Q

Anxiolytics mechanism of action

A

Same as for hypnotics: Benzodiazepines bind to receptor sites that are closely linked to the GABA-A receptor, inducing a conformational change that enhances the action of the inhibitory neurotransmitter GABA

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12
Q

Most commonly used anxiolytics?

A

Benzodiazepines

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13
Q

Examples of anxiolytics

A

Diazepam
Lorazepam
Chlordiazepozide
Oxazepam

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14
Q

SE’s, cautions/ contraindications anxiolytics

A

Same as hypnotics

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15
Q

Antipsychotics (‘neuroleptics’) mechanism of action

A

Blockade of CNS dopamine (D2) receptors
Extra info:
There are 3 main dopaminergic pathways in the CNS. The mesolimbic pathway runs between the midbrain and the limbic system/frontal cortex. D2 blockade in this pathway is probably the main determinant of antipsychotic effect.
D2 receptors are also found int he chemoreceptor trigger zone, where blockade accounts for their use in nausea and vomiting

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16
Q

Antipsychotics indications

A

ST - quieten disturbed pts whatever underlying psychopathology e.g. schizophrenia, mania, toxic delirium
LT - management of schizophrenia, intractable hiccup, nausea and vomiting

17
Q

Examples of antipsychotics

A

Haloperidol
Chlorpromazine
Prochlorperazine

18
Q

SE’s antipsychotics (7)

A
  1. Extrapyramidal effects - movement abnormalities that arise from D2 blockade in the nigrostriatal pathway
  2. Acute drowsiness
  3. Hypotension
  4. Tachycardia
  5. Convulsions
  6. Antimuscarinic symptoms (dry mouth, constipation, difficulty with micturition, blurred vision)
  7. Neuroleptic malignant syndrome (hyperthermia, fluctuation conscious level, muscular rigidity, autonomic dysfunction)
19
Q

Cautions / contraindications antipsychotics

A
  • elderly particularly sensitive
  • avoid in dementia as increases stroke and death risk
  • use with caution (due to extrapyramidal effects) in parkinsons
    use with caution in: liver disease, renal impairment, CV disease, epilepsy, myasthenia gravis, glaucoma
    Containdication in coma and phaeochromocytoma
20
Q

Drug interactions antipsychotics

A

Many, refer to BNF. Prominent among these are drugs that prolong the QT interval

21
Q

What are antiepileptics

A

Drug of choice for seizure type in adults.

22
Q

Examples of antiepileptics

A

Carbamazepine
Valproate
Phenytoin
Fosphenytoin

23
Q

Carbamazepine (antiepileptic) mechanism of action

A

Inhibition of repetitive neuronal firing is produced by reduction of transmembrane Na+ influx by use-dependent blockade of Na+ Channels

24
Q

Carbamazepine indications

A

Drug of choice for simple and complex partial seizures, and for tonic-clonic seizures secondary to a focal discharge

25
Q

SE Carbamazepine

A

Nausea and vomiting esp in early treatment
CNS toxicity leads to double vision, dizziness, drowsiness and ataxia
Transient leucopenia is common, esp in early treatment
Hyponatraemia caused by potentiation of ADH

26
Q

Contraindications / caustions carbamazepine

A
  • Contraindication in AV conduction abnormalities (unless paced), hx of bone marrow depression, porphyria
  • Hepatic enzyme induction leading to accelerated metabolism of the oral contraceptive pill (dose should be inc)
  • Warfarin (reduced anticoagulant effect),
  • Ciclosporin
27
Q

Valproate (antiepileptic) mechanism of action

A

Blockade of transmembrane Na+ channels, thus stabilising neuronal membranes

28
Q

Valproate indications

A

Effective for all forms of epilepsy

29
Q

SE Valproate

A 
GI upset (nausea, vomiting, anorexia, abdo pain, acute pancreatitis)
Inc appetite and weight gain
Transient hair loss
Dose related tremor
Thrombocytopenia
Rarely severe hepatotoxicity
30
Q

Cautions / contraindications Valproate

A

Acute liver disease
Porphyria
Monitor liver biochemistry 6-monthly in those most at risk of severe liver damage

31
Q

Phenytoin/ Fosphenytoin (antiepileptic) mechanism of action -

A

inhibit sodium influx across the cell membrane, reduce cell excitability

32
Q

Phenytoin/ Fosphenytoin indications

A

all forms of epilepsy except absence seizures, but used much less in developed countries
Also used in management of status epilepticus and in trigeminal neuralgia

33
Q

SE’s Phenytoin/ Fosphenytoin (bloody loads)

A

IV injection may cause CNS, CV (hypotension, heart block, arrhythmias) and resp depression

Other SEs are dose related and include:

  • impaired brainstem and cerebellar function (nystagmus, double vision, vertigo, ataxia, dysarthria)
  • chronic connective tissue effects (gum hyperplasia, coarsening of facial features, hirsutism)
  • skin rashes (withdraw treatment)
  • folate deficiency
  • Increased vit D metabolism and deficiency
  • Blood dyscrasias
  • Lymphadenopathy
  • Teratogenic effects
34
Q

Cautions and contraindications Phenytoin/ Fosphenytoin

A

contraindicated in sinus brachycardia, heart block and porphyria
many drug interactions - BNF
Highly protein bound and can be displaced by valproate and salicylates, which therefore enhance the effect
Induction of hepatic drug-metabolising enzymes and metabolism of warfarin and ciclosporin increased

Neuro (15 decks)

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