Neuromuscular and neurological

Question 1

Levodopa is for

Answer 1

Parkinson’s disease

Question 2

What does Levodopa do?

Answer 2

It’s the precursor of dopamine. Increase brain dopamine (DA) by crossing the BBB and being converted to DA to replenish depleted striata DA. It can be converted in the peripheral tissue so is usually administered with peripheral inhibitors to avoid AEs

Question 3

Levodopa works with

Answer 3

Benserazide, carbidopa and entacapone (inhibit levodopa conversion to dopamine in peripheral tissues because it can’t cross the BBB as dopamine).
Amantadine (stimulate dopamine release)
Selegiline (inhibit the breakdown of dopamine)

Question 4

Benserazide and carbidopa are

Answer 4

Inhibitors of decarboxylase and can’t cross the BBB. Given as fixed-dose combos

Question 5

AEs of Levodopa:

Answer 5

Nausea, vomiting chemoreceptor zone (CTZ), orthostatic hypotension, involuntary movements (head, lips, tongue), agitation and confusion (due to the disease itself) and depression (may require antidepressants).

Question 6

Entacapone is for

Answer 6

Parkinson’s disease

Question 7

What does entacapone do

Answer 7

Inhibits catechol-O-methyltransferase (COMT- metabolises catecholamines like DA and levodopa)

Question 8

Can entacapone cross the BBB

Answer 8

No

Question 9

What does entacapone affect and do

Answer 9

Mainly the peripheral COMT and prolongs the clinical response to levodopa

Question 10

AEs of entacapone:

Answer 10

Nausea and vomiting, diarrhoea, dyskinesia and drug-drug interactions.

Question 11

What is amantadine for

Answer 11

Parkinson’s disease

Question 12

What does amantadine do

Answer 12

It’s an antiviral used against some strains of bacteria. It increases DA release, blocks cholinergic receptors, and acts as an N-methyl-D-aspartate antagonist in the glutamatergic pathway from the subthalamic nucleus to globus pallidus.

Question 13

AEs of amantadine

Answer 13

Nightmares, insomnia, hallucinations, dizziness, orthostatic hypotension and ankle oedema.

Question 14

What is selegiline for

Answer 14

Parkinson’s disease

Question 15

What is selegiline

Answer 15

A MAO type B inhibitor (MAO-B). Inhibition of MAO-B activity increase DA levels and may also block DA re-uptake. MAO-B is an enzyme that degrades DA particularly in the SN (serotoninergic neurons)

Question 16

Selegiline is used with

Answer 16

Smaller doses of levodopa

Question 17

AEs of selegiline

Answer 17

Dry mouth and a transient increase in liver enzymes

Question 18

Medications of multiple sclerosis (MS) are for

Answer 18

Controlling symptoms (depression, spasticity). Antidepression for depression, diazepam for spasticity

Question 19

For management of acute relapses of MS

Answer 19

Corticosteroids (PO or IV). E.g. methylprednisolone (IV) to shorten duration of acute relapse by inhibiting mediator synthesis, mast cell de-granulation, increases WBC, and fibroblasts and thus improves nerve conduction.

Question 20

Interferon beta and glatiramer used for and what does it do

Answer 20

For MS and it’s to minimise disease progression, reduce the frequency of relapses, promote myelination, prevent de-myelination and disability.

Question 21

How does interferon beta work?

Answer 21

It has an immunoregulatory action, thus decreases cytokine release, augments suppressor T cell function and increases the activity of macrophages and cytotoxic T cells

Question 22

AEs of interferon beta

Answer 22

Influenza-type signs and symptoms that decrease with continued therapy (fever, joint, muscle pain, headache) and injection site reaction

Question 23

How does glatiramer work?

Answer 23

Pharmacodynamics are poorly understood but it is thought that it blocks presentation of myelin antigens to T cells and induces suppressor T cells

Question 24

AEs of glatiramer

Answer 24

Local effects (redness, pain, itching) and systemic effects (chest pain, palpitations, flushing)

Question 25

What is fampridine for and what does it do?

Answer 25

For MS. A K+ channel blocker (SR, BD). It restores conduction in demyelinated axons by reducing current leakage from demyelinated neurons and thus improves walking speed.

Question 26

Who is fampridine contraindicated in?

Answer 26

People with a history of seizures and renal insufficiency

Question 27

AEs of fampridine:

Answer 27

Insomnia, dizziness, headaches and urinary tract infection (UTI)

Question 28

What are anticholinesterases like neogesigmine (SC/IM) and pyridostigmine (oral) for and what do they do.

Answer 28

For myasthenia gravis. Help reduce degradation of ACh by inhibiting cholinesterase and enhances neuromuscular transmission. Thus, more ACh is available and its action is prolonged

Question 29

AEs of anticholinesterases like neogesigmine and pyridostigmine:

Answer 29

Increased salivation, nausea, vomiting and diarrhoea

Question 30

Corticosteroids for myasthenia graves used to

Answer 30

Decrease inflammation

Question 31

Immunosuppressants for myasthenia gravis:

Answer 31

Ciclosporin and azathioporine

Question 32

What does ciclosporin do

Answer 32

It’s a calcineurin inhibitor- it blocks the action of calcineurin in activated T cells. It prevents production of interleukin-2 and other cytokines which normally stimulate T cell proliferation and differentiation.

Question 33

AEs of ciclosporin

Answer 33

GI disturbances and hirsutism

Question 34

What does azathioprine do

Answer 34

Impairs lymphocyte proliferation, cellular immunity and antibody response

Question 35

AEs of azathioprine

Answer 35

Thrombocytopenia, anaemia and leucopenia. Susceptibility to infection as well as liver and kidney dysfunction in higher doses.