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Pharmacology Flashcards

1
Q

Rivastigmine

A

Cholinesterase inhibitor. Used in dementia. Prevents ACh breakdown.
ADE: GI distress/muscle cramps, abnormal dreams. CAUTION in Bradycardia.
6-12 month delay in progression.

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2
Q

Donepezil

A

Cholinesterase inhibitor. Used in dementia. Prevents ACh breakdown.
ADE: GI distress/muscle cramps, abnormal dreams. CAUTION in Bradycardia.
6-12 month delay in progression.

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3
Q

Memantine

A

NMDA antagonist, prevents glutamate induced excitotoxicity. Used in dementia. Can be combined with AChi

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4
Q

Levopoa

A

Used in PD.
Converts to DA.
ADE: N&V (treat with domperidone), hypotension, dyskinesias, increased suicide risk, impulse issues. At high dose hallucinations, psychosis and confusion (can treat with non-dopaminergic antipsychotics (clozapine, quietapine).

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5
Q

Carbidopa

A

Dopa decarboxylase inhibitor.
Used in PD to enhance L-Dopa by blocking L-Dopa to DA conversion peripherally.
Combo is co-careldopa

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6
Q

Benserazide

A

Dopa decarboxylase inhibitor.
Used in PD to enhance L-Dopa by blocking L-Dopa to DA conversion peripherally.
Combo is co-beneldopa

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7
Q

Entecapone/tolcapone

A

COMT inhibotr. Used in PD. Blocks DA breakdown in peripherly/CNS, also blocks L-DOPA - > 3-OMD conversion

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8
Q

selegiline

A

MAO-B inhibitor. Blocks DA breakdown in CNS. Used for PD. very view ADEs, but at high doses loses selectivity and affects MAO-A

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9
Q

Rasagiline

A

MAO-B inhibitor. Blocks DA breakdown in CNS. Used for PD. very view ADEs, but at high doses loses selectivity and affects MAO-A

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10
Q

Pramipexole, ropinirole (Bromocriptine is older)

A 
Dopamine antagonist (D2/D3). Used in PD. Can work even when more dopaminergic neurons are lost. 
ADE: drowsiness, hallucinations, compulsive behaviours
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11
Q

Procyclidine

A

Muscarinic antagonist, was used in PD but less so now as poorly tolerated.
ADEs: antimuscarinic (dry motuth, blurred vision, urinary retention)

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12
Q

Diazepam

A

Benzodiazepine. Allosteric GABA modulator that increases GABA. Used in epilepsy (anticonvulscant). Acts quickly (rectal, buccal, oral, IV). ADEs: dependence, withdrawal, tolerance, sedation

Can also be used for anxiety Only work if GABA present. Can be used as muscle relaxant, anticonvulsant, amnesia (flunitrazepam), sedative, anxiolytic (acute use only)

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13
Q

Tiagabine

A

Inhibits GABA transaminase (increases GABA). Anticonvulsant. Add on therapy for partial seizure
ADE: drowsiness, confusion, dizziness.

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14
Q

Vigabatrin

A

GABA-AT inhibitor, increases GABA by inhibiting catabolism

Last resort anti-epileptic. Rarely causes irreversible peripheral visual field defect (needs screening)

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15
Q

Phenytoin (just class)

A

Sodium channel blocker

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16
Q

Valproate (just class)

A

Sodium and calcium channel blocker, teratogen

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17
Q

Carbamazepin (just class)

A

Sodium channel blocker

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18
Q

lamotrigine (just class)

A

Sodium channel blocker

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19
Q

Ethosuximide (just class)

A

Calcium channel blocker

20
Q

Sodium channel blockers

A

Anticonvulsant. Blocks rapidly firing sodium channels. Used for all seizures except absence
ADEs: rash.

21
Q

Calcium channel blockers

A

Anticonvulsants.
Block T type calcium channels, these determine rhthmic discharge of thalamic neurons - absence seizures.
Only for absence seizures as exacerbate tonic-clonic

22
Q

Amitriptyline

A

TCA antidepressant. Blocks NA and 5HT reuptake.
ADEs: antimuscarinic (dry mouth, urinary retention, constipation, impotence, blurred vision), antihistamine (confusoin/sedation), postural hypotension, seizures. Risk of long QT (sudden death). Dangerous with alcohol and OD risk

23
Q

Fluoxetine

A

SSRI, blocks 5-HT reuptake.
ADEs: N&V, diarrhoea, insomnia. Can cause prolonged QT (sudden cardiac death). Not recommended in children, not to be combined with MAOis. Can inhibit metabolism of other drugs through CYP450

24
Q

sertraline

A

SSRI, blocks 5-HT reuptake.
ADEs: N&V, diarrhoea, insomnia. Can cause prolonged QT (sudden cardiac death).Not recommended in children, not to be combined with MAOis. Can inhibit metabolism of other drugs through CYP450

25
Q

Citalopram

A

SSRI, blocks 5-HT reuptake.
ADEs: N&V, diarrhoea, insomnia. Can cause prolonged QT (sudden cardiac death).Not recommended in children, not to be combined with MAOis. Can inhibit metabolism of other drugs through CYP450

26
Q

Velafazine/duloxetine

A

SNRI. Block 5-HT and NA reuptake. Cause sedation and dizziness. Low OD risk. Can inhibit metabolism of other drugs through CYP450. Do not combine with MAO-Ai

27
Q

St John’s wort

A

SNRI. Block 5-HT and NA reuptake. Cause sedation and dizziness. Low OD risk. Can inhibit metabolism of other drugs through CYP450. Do not combine with MAO-Ai

28
Q

Lofepramide

A

NRI, blocks NA reuptake.
ADEs: headache, dry mouth, insomnia. \

Used for depression associated with anxiety.

29
Q

Moclobemide

A

MAOi (selective). Inhibits MAO, preventing NA, 5-HT and DA breakdown in neurons.
CI with tyramine containing foods, do not combine with SSRIs, SNRIs

30
Q

Mirtazepine

A

Monoamine receptor antagonist (alpha 2(NA) and 5HT2c (histamine) receptor antagonist. NA, and 5-HT increase (as targets presynaptic receptor)

31
Q

Bupropion

A

Inhibits Na and DA reuptake

32
Q

Agomelantine

A

Melatonin agonist. Used for severe depression

33
Q

Ketamine

A

NMDA blocker (non competitive), trials for depression

34
Q

Chlorpromazine

A

D2 antagonist - antipsychotic. ADEs: Sedation, weight gain, akinesia, extrapyramidal (acute dystonia (readily reversible), tardive dyskinesia (not as reversible), hyperprolactinaemia. Increased risk of DM and CVD. Idiosynchratic ADEs: agranulocytosis (acute leukopenia - needs monitoring). Antipsychotic malignant syndrome, jaundice

35
Q

Haloperidol

A

D2 antagonist - antipsychotic. ADEs: Sedation, weight gain, akinesia, extrapyramidal (acute dystonia (readily reversible), tardive dyskinesia (not as reversible), hyperprolactinaemia. Increased risk of DM and CVD. Idiosynchratic ADEs: agranulocytosis (acute leukopenia - needs monitoring). Antipsychotic malignant syndrome, jaundice

Much more potent than chlorpromazine

36
Q

Clozapine

A

Atypical antipsychotic. D2 antagonist with less extra pyramidal effects. ADEs: Sedation, weight gain, akinesia, , hyperprolactinaemia. Increased risk of DM and CVD. Idiosynchratic ADEs: agranulocytosis (acute leukopenia - needs monitoring). Antipsychotic malignant syndrome, jaundice

Clozapine has more risk of agranulocytosis - but is good for 1/3 of patients who don’t respond to other therapy.

37
Q

Risperidone

A

Atypical antipsychotic. D2 antagonist with less extra pyramidal effects. ADEs: Sedation, weight gain, akinesia, , hyperprolactinaemia. Increased risk of DM and CVD. Idiosynchratic ADEs: agranulocytosis (acute leukopenia - needs monitoring). Antipsychotic malignant syndrome, jaundice

38
Q

Olazepine

A

Atypical antipsychotic. D2 antagonist with less extra pyramidal effects. ADEs: Sedation, weight gain, akinesia, , hyperprolactinaemia. Increased risk of DM and CVD. Idiosynchratic ADEs: agranulocytosis (acute leukopenia - needs monitoring). Antipsychotic malignant syndrome, jaundice

39
Q

Quietiapine

A

Atypical antipsychotic. D2 antagonist with less extra pyramidal effects. ADEs: Sedation, weight gain, akinesia, , hyperprolactinaemia. Increased risk of DM and CVD. Idiosynchratic ADEs: agranulocytosis (acute leukopenia - needs monitoring). Antipsychotic malignant syndrome, jaundice

40
Q

Aripiprazole

A

Antipsychotic. Partial dopamine agonist. Gives 20-25% of DA effect. Has higher effinity for D2<5HT2A.
Fewer ADEs than others, causes sedation

41
Q

5HT2A pathway significance?

A

Nigrostriatal dopaminergic pathway, involved in extrapyramidal ADEs, aripiprazole avoids this as has less affinity.

42
Q

Buspirone

A

5HT1A partial agonist. Anxiolytic. 5HT1A are pre and post synaptic in corticolimbic system (emotional behaviour). agonism causes initial 5HT drop, then desensitises causes 5HT increase. ADEs: nausea, dizziness, headache. Used for generalised anxiety, not phobias. Has slow onset, little sedation, withdrawal, or alcohol effects.

43
Q

Zopiclone, zolpidem

A

Z drugs. Hypnotic. Anxiety drug.

Act as benzodiazepine receptor, but different structure - selective for alpha1 subunit receptors

44
Q

Bipolar disorder medication

A

Lithium + antiepileptic/antipsychotic .
Can combine with carbamazepine, valproate and lamotrigine (sodium channel blockers) or with olanzapine, quietepine and aripiprazole.
Haloperidol can also be used.
Olanzapine can be given with lithium or valproate.

45
Q

MS RRMS

A

DMT FLT : interferon (1-b/1-a) and glatiramer acetate (daily/weekly subcut injection
Teriflunomide (oral tablets). ADEs GI problems, LF impairment (LFT blood tests needed), lymphocytopenia, allergy
Dimethylfumarate (oral) ADEs: flushing, GI events (often on treatment onset, may come back). Better ADE profile to teriflunomide.
During relapse, can use natalizumab (monoclonal antibody blocking WBC with VCAM1, prevents BBB access to WBCs), fingolimod (depletes peripheral lymphocytes in lymph nodes, therefore less to enter CNS - oral treatment. ADEs bradycardia, immunosuppression, minor BP increase, may have basal cell carcinoma/melanoma association), alemtuzumab (binds B and T cells to modulate immune system. Uses IV infusion for 2x courses, monthly monitoring required for immune function. ADEs: thrombocytonpenia, thyroid disease, nephropathies, rash, headache, fever, resp infection)
Can also use steroids during relapse (IV/oral methylprednisolone)

46
Q

PPMS/SPMS

A

SPMS clinical trial for sponimod, PPMS clinical trial for ocrelizumab.
Can manage spasticity with baclofen, botulinum, tizanidine, sativex
Can manage neuropathic pain with Gabapentin, pregabalin, amitriptyline, carbamazepine
Can manage fatigue with amantadine, modafinil
Can manage neurogenic bladder with antichlolinergic treatment (oxybutynin, tolterodine, solifenocin, mirabegron)

Neuro (6 decks)

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