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Pharmacology > Drugs Affecting the CNS > Flashcards

Drugs Affecting the CNS Flashcards

1
Q

Valerian & Motherwort

A

Pharmacodynamics: GABA-A agonists;
Indications for use: Plant derived decreasing stimulation in
the CNS, Used as anxiolytics (anxiety, panic,
phobia, PTSD and aggression) and as sedatives in sub-hypnotic and hypnotic doses without the hypnotic effect. Can also cause central myo-relaxation.

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2
Q

How does GABA inhibit AP?

A

Binds to GABA binding site or binds to other subunits to increase affinity to GABA and opens Cl- ion channel (increases frequency or duration).

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3
Q

Carvalol (Valerian + Phenobarbital)

A

Pharmacodynamics: GABA - A agonist (combined barbiturate and plant derivative);
Indications for use: same as plant derived tranquillisers.

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4
Q

Phenazepam & Nitrazepam

A

Pharmacodynamics: (Benzodiazepines) GABA-A agonists;
Indications for use: Used as anxiolytics and as sedatives / hypnotic. Can be used to treat anxiety disorders, sleep disorders.

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5
Q

Diazepam & Clonazepam

A

Pharmacodynamics: (Benzodiazepines) GABA-A agonists;
Indications for use: Used as anxiolytics and as sedatives / hypnotic and treats seizures. Diazepam treats muscular disorders such as multiple sclerosis.

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6
Q

Chlordiazepoxide, Gidazepam (Atypical), Medazepam, Bromisoval

A

Pharmacodynamics: (Benzodiazepines) GABA-A agonists;

Indications for use: Used as anxiolytics and as sedatives / hypnotics.

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7
Q

Phenobarbital

A

Pharmacodynamics: (Barbiturate) GABA-A agonists;

Indications for use: Used as anxiolytics and as sedatives / hypnotic.

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8
Q

Zopiclone (Imovane)

A

Pharmacodynamics: (Benzodiazepines) GABA-A agonist (a1 subunit);
Indications for use: Used as anxiolytics and as sedatives / hypnotic, drug of choice as safe to stop drug abruptly - no withdrawal symptoms.

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9
Q

Haloperidol & Droperidol

A

Pharmacodynamics: Dopamine antagonists;
Indications for use: Neuroleptic D2 blockers in mesolimbic and mesocortical systems cause antipsychotic effect. In vomiting centre has an anti-emitic effect.

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10
Q

Orphenadrine, Biperiden, Procyclidine, Trihexyphenidyl and Benzotropine

A

Pharmacodynamics: mACh blocker;
Indications for use: decreases extrapyrimidal
effects associated with Parkinson’s and a result of anti-psychotics.

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11
Q

Trifluoperazin

A

Pharmacodynamics: Dopamine antagonist, mACh and α1 blocker;

Indications for use: used as an antipsychotic, reduces extra-pyramidal effects and reduced sympathetic tone.

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12
Q

Sulpride, Chlorpromazine (aminazine) and Clorprothixene

A

Pharmacodynamics: Mixed blocker / antagonist (D, 5-HT, H, α, mACh);
Indications for use: Typical neuroleptics –> antipsychotic affect, sedation, anti-emitic.

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13
Q

Doxylamine

A

Pharmacodynamics: H1 blocker;

Indications for use: treats schizophrenic patients by inducing sedation.

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14
Q

What are the side effects of Benzodiazepines?

A

Lack of tolerance causing: sedation, memory impairment, lack of concentration, motor incoordination, muscle weakness and acute confusion. Can also cause physical dependence and withdrawal symptoms include insomnia, anxiety, apprehension, irritability, palpitations, tremor, vertigo and sweating.

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15
Q

What are the contraindication of Benzodiazepines?

A

Not to be taken with other sedatives, with alcohol or by those with respiratory distress. Not to be used by those who will be driving, operating heavy machinery or need to be alert.

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16
Q

What are the side effects of hypnotics?

A

Pharmacodynamic tolerance leads to decreased effect but no increased tolerance to lethal effect. Abused. Dependence. Lack of energy. Anterograde amnesia.
Increased reaction time. Impairment of motor and mental function. Confusion.

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17
Q

What are the contraindications of hypnotics?

A

Patients with sleep apnoea; Not to be taken with

alcohol; Should not be used by pregnant women or by those who need to be alert at night.

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18
Q

Contraindications of neuroleptics?

A

Liver damage; Coronary artery disease; Cerebrovascular

disease; Parkinsonism; Bone marrow depression; Sever hypotension or hypertension; Severe depression.

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19
Q

Side effects of alpha 1 antagonists?

A

Alpha 1 antagonist – vasodilation, decreasing BP causing orthostatic collapse.

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20
Q

Side effects of H1 antagonists?

A

Common side effects include: drowsiness, dry mouth, dizziness, constipation or difficulty urinating and stomach upset.

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21
Q

Side effects of 5-HT antagonists?

A

5-HT receptor blocking – Increases appetite leading to weight gain.

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22
Q

Side effects of mACh antagonists?

A

mACh blocking – increases intraocular pressure, decreases gland secretion (dry mouth), relaxes smooth muscle causing constipation.

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23
Q

Phenytoin (Diphenin), Carbamazepine, Lamotrigine (Lamictal), Sodium Valproate (Depikine), Topirimate, Rufinamide, Lacosamide

A

Pharmacodynamics: Voltage-dependent sodium ion channel blocker;
Indications for use: Used to reduce inappropriate focal
discharge (seizures) by blocking of voltage dependent / gated sodium ion channels.

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24
Q

Zonisamide

A

Pharmacodynamics: Voltage dependent sodium ion channel and T type calcium channel blocker;
Indications for use: Reduces inappropriate focal discharge (seizures).

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25
Q

Ethosuximide, Gabapentin, Pregabalin

A

Pharmacodynamics: T-type calcium channel blockers;

Indications for use: Reduces inappropriate focal discharge (seizures).

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26
Q

Felbamate

A

Pharmacodynamics: Voltage dependent sodium ion channel blocker and GABA-A agonist;
Indications for use: Reduces inappropriate focal discharge (seizures).

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27
Q

Vigabatrin

A

Pharmacodynamics: inhibits GABA transaminase reducing degradation of GABA;
Indications for use: Reduces inappropriate focal discharge (seizures).

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28
Q

Levitaracetam

A

Pharmacodynamics: binds to SVA2 which regulates
trafficking of Syt involved in calcium response and also
involved in modulating GABA release in the hippocampus;
Indications for use: Reduces inappropriate focal discharge (seizures).

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29
Q

Tigabine

A

Pharmacodynamics: Inhibits GABA uptake;

Indications for use: Reduces inappropriate focal discharge (seizures).

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30
Q

Retigabine

A

Pharmacodynamics: Activates KCNQ2 potassium channels;
Indications for use: Reduces inappropriate focal discharge (seizures);
Clinical features: prolongs QT interval may provoke ventricular arrhythmia and weight gain.

31
Q

Perampanel

A

Pharmacodynamics: (Non-competetive AMPA antagonist)
Indications for use: Reduces inappropriate focal discharge (seizures);
Side effects: Dizziness, weight gain, sedations, impaired coordination, changes in mood and behaviour.

32
Q

Cinnarizine

A

Pharmacodynamics: H1, D2, TTVGCC antagonist / blocker;

Indications for use: sedation, used for motion sickness and vertigo.

33
Q

Ropinorole, Pramipexole & Rotigotine

A

Pharmacodynamics: Dopamine agonists;

Indications for use: Reduces the mobility related symptoms associated with Parkinson’s such as Ataxia and bradykinesia.

34
Q

Cabergoline, Pergolide & Bromocriptine

A

Pharmacodynamics: Dopamine agonists;
Indications for use: Reduces the mobility related symptoms associated with Parkinson’s such as Ataxia and bradykinesia;
Clinical features: Limited by side effects: nausea, vomiting,
somnolescence, fibrotic reactions in the lungs / retroperitoneum / pericardium.

35
Q

Uses Selegeline, Safinimide, Rasagiline

A

Pharmacodynamics: MAO-B inhibitors;
Indications for use: reduce re-uptake and destruction of dopamine and therefore increase dopamine available in Parkinson’s patients to reduce mobility related symptoms.

36
Q

Fluoxetine (Prozac), Fluvoxamine, Paroxetine (Paxil), Sertraline (Zoloft), Citalopram, Escitalopram & Vilazadone

A

Pharmacodynamics: MA uptake inhibitors (Selective Serotonin Reuptake Inhibitors (SSRIs);
Indications for use: Used to relieve depressive symptoms (antidepressant).

37
Q

Imipramine (Melipramine, Imizine), Desimpramine, Amitriptyline, Nortryptiline and Clomipramine

A

Pharmacodynamics: MA uptake inhibitors (Classic Tricyclic
Antidepressants (CTAs));
Indications for use: Used to relieve depressive symptoms (antidepressant).

38
Q

Venlafaxine, Desvenlafaxine, Duloxetine and Sibutramine

A

Pharmacodynamics: MA uptake inhibitor (Mixed 5-HT and NA reuptake inhibitors);
Indications for use: Used to relieve depressive symptoms (antidepressant).

39
Q

Bupropion, Reboxetine, Atomoxetine and Maprotiline (Ludiomil)

A

Pharmacodynamics: MA uptake inhibitor (Noradrenaline Reuptake Inhibitor);
Indications for use: Used to relieve depressive symptoms (antidepressant).

40
Q

St John’s Wart

A

Pharmacodynamics: MA uptake inhibitor (Herbal);

Indications for use: Used to relieve depressive symptoms (antidepressant).　

41
Q

Phenelzine, Iproniazid, Nialimide and Tranylcypromine

A

Pharmacodynamics: MAOI (Irreversible non-competitive inhibitor);
Indications for use: Used to relieve depressive symptoms (antidepressant);　
Clinical features: Phen and Ip Can cause hepatotoxicity so contraindicated in patients with hepatic impairment.

42
Q

Moclobemide

A

Pharmacodynamics: Reversible MAO-A selective inhibitor;

Indications for use: Used to relieve depressive symptoms (antidepressant).　

43
Q

Agomelatine

A

Pharmacodynamics: Melatonin Receptor agonists;
Indications for use: Regulates circadian rhythm and eliminates insomnia related to depression;
Clinical features: Can cause hepatotoxicity so not be used in patients who are hepatically impaired.

44
Q

Levodopa

A

Pharmacodynamics: Is a pro-drug of dopamine;
Indications for use: Used in Parkinson’s to reduce mobility related symptoms;
Clinical features: To counteract nausea a dopamine antagonist that works in the chemoreceptor trigger zone but does not penetrate the basal ganglia can be used: Domperidone. Due to the fluctuation of plasma concentration in short acting agonists such as Levodopa dyskinesia can develop as a side effect. Can also lead to postural hypotension. Can cause schizophrenic like symptoms.

45
Q

Apomorphine

A

Pharmacodynamics: Dopamine agonist;
Indications for use: controls the off effect of Levodopa but has an emitic effect so has to be taken with anti-emitic. Can also cause mood and behavioural changes, cardiac disrhythmias and hypotension.

46
Q

Modafinil

A

Pharmacodynamics: NMDA antagonist;
Indications for use: Nootropics: NMDA antagonists beneficial in reducing brain damage after strokes and head injury. Treats epilepsy, Alzheimer’s and ADHD. “Wakefulness promoting agent”.

47
Q

Memantine

A

Pharmacodynamics: NMDA antagonist;
Indications for use: Nootropics: NMDA antagonists beneficial in reducing brain damage after strokes and head
injury. Treats epilepsy, Alzheimer’s and ADHD. Lipid soluble.

48
Q

Phencyclidine

A

Pharmacodynamics: NMDA antagonist;
Indications for use: Nootropics: NMDA antagonists beneficial in reducing brain damage after strokes and head
injury. Treats epilepsy, Alzheimer’s and ADHD. Lipid soluble.

49
Q

Ketamine

A

Pharmacodynamics: NMDA antagonist;
Indications for use: Nootropics: NMDA antagonists beneficial in reducing brain damage after strokes and head
injury. Treats epilepsy, Alzheimer’s and ADHD. Clinical features: Used in treatment of depression as an anaesthetic and as analgesia. Can cause hypertension, tachycardia and hypersalivation. Lipid soluble.

50
Q

Kynurenic acid / 7 – chloro-kynurenic acid

A

Pharmacodynamics: NMDA antagonist (Blocks glycine site where NMDA binds);
Indications for use: Nootropics: NMDA antagonists beneficial in reducing brain damage after strokes and head
injury. Treats epilepsy, Alzheimer’s and ADHD.

51
Q

Amphetamine

A

Pharmacodynamics: Increases dopamine, NA and 5-HT (effect).

Indications for use: used for ADHD.

52
Q

Glycine

A

Pharmacodynamics: stimulates ACh release;
Indications for use: beneficial in reducing brain damage after strokes and head injury. Treats epilepsy, Alzheimer’s and ADHD.

53
Q

Donepezil, Galantamine, Rivastigmine and Tacrine

A

Pharmacodynamics: Acetylcholine esterase inhibitors;

Indications for use: Slows progression of Alzheimer’s as may reduce the formation of amyloid beta.

54
Q

Methylphenidate

A

Pharmacodynamics: Norepinephrine – dopamine reuptake
inhibitor;
Indications for use: Treatment of ADHD.

55
Q

Nimodipine (Nimotop)

A

Pharmacodynamics: Calcium Channel Blocker (nootropic);

Indications for use: reducing vasospasm related to ischaemia in subarachnoid haemorrhage.

56
Q

Vinpocetin (Cavinton)

A

Pharmacodynamics: sodium channel blocker (nootropic);

Indications for use: used to treat cerebrovascular incidents to improve cognition post CI;

57
Q

Nicergoline (Sermion)

A

Pharmacodynamics: a1 antagonist (nootropic);

Indications for use: decreases vascular resistance increasing oxygen and glucose utilisation.

58
Q

Pentoxifyline (Trental)

A

Pharmacodynamics: phosphodiesterase inhibitor increasing cAMP (nootropic);
Indications for use: reducing the effects of innate immunity, decreasing clotting and therefore viscosity, relieving pain in intermittent claudication.

59
Q

Phenibut (Noofen)

A

Pharmacodynamics: GABA-B agonist;
Indications for use: causing CNS depression
indicated for use in depression and alcohol withdrawal.

60
Q

Pantogam (Hopantenic acid)

A

Pharmacodynamics: GABA agonist pro drug;

Indications for use: indicated for psychiatric disorders.

61
Q

What are the side effects of SSRIs?

A

Nausea, loss of appetite, insomnia, loss of libido and failure to orgasm, possible increased aggression and violence (Fluoxetine).

62
Q

What are the contraindications of SSRIs?

A

When used with MAOIs can cause serotonin syndrome (tremor, hyperthermia, cardiovascular collapse) in under 18s excitement, insomnia, aggression, suicidal ideation.

63
Q

What are the side effects of TCAs?

A

Sedation, confusion, motor incoordination. Anti-muscarinic effects: dry mouth, blurred vision, constipation and urinary retention, postural hypotension, increased QT interval.

64
Q

What are the contraindication of TCAs?

A

Metabolised by CP450 so elimination interference by
other hepatically metabolised drugs. Interacts with alcohol and anaesthetics (pathway unknown), interacts with hypertensive drugs.

65
Q

Clozapine

A

Pharmacodynamics: 5-HT blocker;
Indications for use: Atypical antipsychotic reduces suicidal tendencies and used when treatment with other more common drugs is insufficient.

66
Q

What are the side effects of (Wolf of) Dopamine agonists?

A

The side effects are somnolescence, hallucinations, compulsion to engage in risky behaviour (gambling, over-eating and sexual excess).

67
Q

Amantadine

A

Pharmacodynamics: NMDA type glutamate receptor antagonist, increases dopamine releases and blocks reuptake, anticholinergic;
Indications for use: treats the dyskinesia caused by levodopa as it stabilises the close state of NMDA receptors. (PD)

68
Q

Piracetam

A

Pharmacodynamics: NMDA receptor antagonist, an AMPA agonist improving function of ACh;
Indication for use: Nootropics: NMDA antagonists beneficial in reducing brain damage after strokes and head
injury. Treats epilepsy, Alzheimer’s and ADHD.

69
Q

What are the common side effects of mixed 5-HT and NA inhibitors?

A

The common side effects are headache, insomnia, sexual dysfunction, dry mouth, dizziness, sweating, decreased appetite.

70
Q

What are the contraindication of mixed 5-HT and NA inhibitors?

A

The contraindications of mixed 5-HT and NA inhibitors are that as it can cause hepatotoxicity it is contraindicated for
patients with hepatic impairment.

71
Q

What are analeptic drugs used for?

A

Analeptic drugs: are central nervous system
stimulants that treat depression, ADHD, respiratory depression and therefore useful for anaesthetic recovery and treating barbiturate overdose.

72
Q

Which analeptic act on the cortex?

A

Caffeine

73
Q

Which analeptic acts on the medulla?

A

Aethimizol, Cardiamine, Bemegride, Sulfocamphocaine, Carbogen.

74
Q

Which analeptic acts on the spinal cord?

A

Stritchnine

Pharmacology (11 decks)

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