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Core Conditions > Neuro drugs > Flashcards

Neuro drugs Flashcards

1
Q

Used in the treatment of idiopathic PD, symptomatic parkinsonism, CO intoxication, and restless leg syndrome

A

Madopar/Sinemet

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2
Q

L-DOPA/ peripheral decarboxylase inhibitors

A

Madopar/ Sinemet

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3
Q

Side effects of L-DOPA (3)

A

Dyskinesias, involuntary movements and nausea
Mostly due to activity of dopamine
Reactions can be reduced by lower dose

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4
Q

Contraindications of L-DOPA (2)

A

Narrow angle glaucoma

Suspicious undiagnosed skin lesions of Hx of melanoma (may activate malignant melanoma)

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5
Q

How does L-DOPA cross the BBB?

A

Precursor to dopamine that is able to cross BBB

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6
Q

How does L-DOPA become activated?

A

Converted to dopamine in the periphery AND the CNS by aromatic-L-amino-acid decarboxylase

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7
Q

L-DOPA is administered with which drug to inhibit activation in the peripheries

A

Dopamine decarboxylase inhibitor (DCC) e.g. Carbidopa

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8
Q

Excretion of L-DOPA

A

Renal (70-80%)

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9
Q

Metabolism of L-DOPA

A

95% in stomach, lumen of intestine, kidney, liver and brain

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10
Q

Interactions of L-DOPA (4)

A

Antihypertensives: increase risk of postural hypotension
Antidepressant (TCAs): Hypertension and dyskinesia
Anticholinergics: affect absorption and pt. response
Iron: decrease bioavailability of carbidopa and/or levodopa

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11
Q

Control of seizure in status epilepticus when BZDs are ineffective, and to reduced generalised or focal seizures in epilepsy

A

Phenytoin

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12
Q

Side effects of long-term phenytoin Rx

A

Change in appearance - skin thickening, acne, hirsutism, gum hypertrophy

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13
Q

Dose-related side effects of phenytoin (3)

A

Neurological effects: cerebellar toxicity (nystagmus, ataxia and disco-ordination) and impaired cognition and consciousness

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14
Q

Phenytoin causes haematological disorders and osteomalacia by inducing the metabolism of ______ and _____

A

Folic acid and vitamin D

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15
Q

Phenytoin toxicity can cause death through what mechanisms?

A

Cardiovascular collapse and respiratory depression

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16
Q

What is the therapeutic index of phenytoin?

A

Narrow - increased concentration causes arrhythmia and cerebellar syndrome

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17
Q

Exposure to phenytoin in utero causes what? What can be done to avoid this?

A

Craniofacial abnormalities and reduced IQ - foetal hydantoin syndrome
Women planning pregnancy should take high-dose folic acid prior to contraception

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18
Q

MoA of phenytoin

A

Reduces neuronal excitability and electrical conductance amongst brain cells, inhibiting the spread of seizure activity

Similar effect in cardiac purkinje fibres may account for arrhythmic and cardiotoxic effects

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19
Q

Metabolism of Phenytoin

A

Liver

20
Q

Interactions of phenytoin

A

Enzyme inducer so reduces plasma conc. and efficacy of drugs metabolised by CYP450 enzymes (warfarin, oestrogen, progesterones)
Metabolised by CYP450, so plasma concentration and adverse effects are increased by CYP450 inhibitors e.g. amiodarone, diltiazem and fluconazole
Complex interactions with other anti-epileptics
Efficacy reduced by drugs lowering the seizure threshold (SSRIs, tricyclic ADs, antipsychotics, tramadol)

21
Q

1st line therapy for focal seizures, Rx of trigeminal neuralgia, Rx of bipolar disease in pts. intolerant to other medications

A

Carbamazepine

22
Q

Dose-related side effects of Carbamazepine

A

GI upset

Neurological effects - dizziness and ataxia

23
Q

Hypersensitivity to carbamazepine

A

Affects 10%, manifests in maculo-papular rash

24
Q

Contraindications of carbamazepine in utero

A

Neural tube defects, cardiac and urinary tract abnormalities

Take folic acid prior to contraception to avoid

25
Q

MoA of carbamazepine

A

Inhibition of neuronal Na+ channels, stabilising resting membrane potential and reducing neuronal excitability

26
Q

Treatment efficacy monitoring of carbamazepine

A

Compare seizure frequency before and after stating treatment

27
Q

Metabolism and excretion of carbamazepine

A

Hepatic (CYP3A4)

Urinary and faecal excretion

28
Q

CYP450 interactions of carbamazepine

A

CYP450 inducer, so reduces efficacy of warfarin, oestrogen, progestogens, etc.
Metabolised by CYP450 so plasma conc. and adverse effects are increased by CYP450 inhibitors (e.g. marcolides)

29
Q

1st line Rx of epilepsy for controlled generalised or absence seizures, Rx of bipolar disorder for acute treatment of manic episodes

A

Sodium valproate

30
Q

Neurological side effects of sodium valproate (3)

A

tremor, ataxia, behavioural disturbances

31
Q

Rare side effects of sodium valproate (4)

A

severe liver injury
pancreatitis
bone marrow failure
anti-epileptic hypersensitivity syndrome

32
Q

Advice in utero for sodium valproate

A

Stop taking before conception - more toxic in utero than other anti-convulsants, causes foetal abnormalities

33
Q

MoA of sodium valproate

A

Weak inhibitor of neuronal Na+ channels, stabilising membrane potential and reducing excitability
Also increases brain content of GABA, reducing excitability of neurones

34
Q

Metabolism and excretion of sodium valproate

A

Hepatic metabolism and mitochondrial beta-oxidation

Urinary excretion

35
Q

CYP450 interactions

A

As with other anti-convulsants

& CYP450 inducers (phenytoin, carbapenems) may increase seizure risk

36
Q

Adjunctive treatment of partial seizures in epilepsy and maintenance treatment of bipolar disorder and depression

A

Lamotrigine

37
Q

Side effects of lamotrigine

A

Skin rash: mild, self-limiting to SJS
Clinical worsening and suicide
Renal failure - accumulation of glucuronide metabolite
Psych: aggression, irritability
NS: headache, somnolence, dizziness, tremor, insomnia, agitation

38
Q

MoA of lamotrigine

A

Chemically unrelated to other AEDs - Phenyltriazene
Stabilised presynaptic neuronal membranes by inhibiting sodium current by bind to the inactivated state of the sodium channel
Similar action to local anaesthetics

39
Q

Metabolism and excretion of lamotrigine

A

Hepatic metabolism

Urinary and faecal excretion

40
Q

Drug interactions (2)

A

Hormonal contraceptive: increase clearance of lamortigine - higher maintenance doses required
AEDs: reduction in metabolism - increased concentration

41
Q

Treatment of partial seizures in adults with epilepsy

A

Levetiracetam

42
Q

Side effects of Levetiracetam

A 
AKI
Nasopharyngitis
Somnolence
Headache
Fatigue
Anorexia
Psych. disorders
Vertigo
43
Q

MoA of levetiracetam

A

Stimulation of synaptic vesicle 2a (SV2A), inhibiting NT release
Inhibition of N-type Ca2+ currents and reduction of Ca2+ release from intraneuronal stores

44
Q

Metabolism and excretion of levetiracetam

A

Metabolism: enzymatic hydrolysis of acetamide group, no CYP450 metabolism
Urinary excretion, unchanged

45
Q

Interactions of levetiracetam (2)

A

Probenecid: renal tubular secretion-blocking agent, inhibits renal clearance of primary metabolite
Methotrexate: decreases methotrexate clearance - potentially toxic blood levels - monitor carefully

Core Conditions (5 decks)

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