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Pharmacology > Drugs for Neurodegenerative Diseases > Flashcards

Drugs for Neurodegenerative Diseases Flashcards

1
Q

Drugs that increase Dopamine levels

A 
Levodopa
Carbidopa
Amantadine
Selegiline
Rasagiline
Tolcapone
Entacapone
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2
Q

Levodopa - MoA

A

Increase dopamine levels by increasing the synthesis.

It is converted to dopamine by LAAD and metabolized to 3OMD by COMT. A drug that inhibits LAAD or COMT increases the amount of levodopa that enters brain tissue.

In the brain levodopa is taken up by dopaminergic neurons in the striatum and converted to dopamine by LAAD. Levodopa thereby increases the amount of dopamine released by the neurons in patients with PD, and is serves as a form of replacement thrapy. As the diseases progresses and more dopaminergic neurons are lost, the conversion of levodopa to dopamine therefor declines.

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3
Q

Levodopa - Indication

A

Idiopathic PD
Postencephalitic parkinsonism

Parkisonian symptoms caused by carbon monoxide poisoning, manganese intoxication, or cerebral arteriosclerosis

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4
Q

Levodopa - Adverse effects

A

Nausea and vomiting (when used alone)
Orthostatic hypotension
Cardias dysrhythmias. Adverse effects are reduced with the use of Carbidopa.

Long term; involuntary movements or dyskinesias
Psychotic effects, including hallucination and disoriented thinking
Sedation, agitation, delirium, vivid dreams or nightmares, euphoria after drug adm.

Discoloration of urine, sweat and or saliva
Loss of appetite

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5
Q

Levodopa - Interactions

A

Anticholinergic drugs –> slow levodopa absorption

Nonselective MOAIs inhibit the breakdown of dopamine and sometimes cause hypertensive crisis in patients receiving levodopa

Antipsychotic drugs block dopamine receptors and can reduce the effectiveness of levodopa and exacerbate motor dysfunction

Drugs that promote gastric emptying (antacids) can increase levodopa bioavailibility

Ingestion of high-protein foods can decrease the effectiveness of levodopa because amino acids can reduce the transport of levodopa into the brain

LAAD requires Vitamin B6 (pyridoxine) as a cofactor. For this reason, vitamin B6 supplements may enhance the peripheral decarboxylation of levodopa and shoult not be coadministered with levodopa

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6
Q

Carbidopa - Group + MoA

A

Analoug of levodopa

Inhibits LAAD thereby reducing the conversion of levodopa to dopamine in peripheral tissues and so increases the amount of levodopa that enters the brain

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7
Q

Carbidopa - Indication + Adverse effects

A

PD

Reduces the cardiovascular and GI side effects of Levodopa.

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8
Q

Amantadine - Group + MoA

A

Antiviral drug

Increases dopamine release from nigrostriatal neurons, may also inhibit the reuptake of dopamine by these neurons.

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9
Q

Amantadine - Indication

A

Early or mild cases of Parkinson disease

Prevention and treatment of influenza

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10
Q

Amantadine - Adverse effects

A 
Sedation
Restlessness
Vivid dreams
Nausea
Dry mouth
Hypotension
Livedo reticularis- reddish-blue mottling of the skin with edema
CNS side effects are more common in elderly pat.
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11
Q

Selegiline - Group + MoA

A

Modified phenylethylamine compound

Increase dopamine by inhibiting the breakdown.

Inhibits Monoamine oxidase type B (MAO-B) and thereby prevents the oxidation of dopamine to dihydroxyphenylacetic acid and hydrogen peroxide. By this selegiline increases dopamine levels in the basal ganglia and decreases the formation of hydrogen peroxide. In the presence of iron, hydrogen peroxide is converted to hydroxyl and hydroxide free radicals that may participate in the degeneration of nigrostriatal neurons in patients with PD.

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12
Q

Selegiline - Indication

A

Early or mild PD
Adjunct with levodopa for advanced disease, reduces the dose of levodopa needed, and may improve motor function in patients who experience wearing-off and on-off difficulties.

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13
Q

Selegiline + Rasagiline - Adverse effects

A 
Confusion
Dyskinesia
Hallucinations
Hypotension
Insomnia
Nausea.
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14
Q

Selegiline + Rasagiline - Interactions

A

Severe reactions may result if taken with meperidine or with fluoxetine or other SSRIs

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15
Q

Rasagiline - MoA

A

MAO-B inhibitor

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16
Q

Rasagiline - Indication

A

Monotherapy or adjunct medication in the treatment of parkinsonism

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17
Q

Tolcapone and Entacapone - MoA

A

Enhances the effectiveness of levopoa by inhibiting COMT, the enzyme that metabolize levodopa to 3OMD. By this action, it produces twofold increase in the oral bioavailability and half-life of levodopa.

Tolcapone: inhibits COMT in glial cells and inhibits conversion of dopamine to 3-methoxytyramine

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18
Q

Tolcapone and Entacapone - Indication

A

PD

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19
Q

Tolcapone and Entacapone - Adverse effects

A 
Both:
Diarrhea
Nausea
Discoloration of urine, sweat, saliva
Tolcapone:
Rare: fatal hepatitis
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20
Q

Dopamine receptor agonists

A 
Bromocriptine
Pramipexole
Ropinirole
Rotigotine
Apomorphine
Benztropine
Trihexyphenidyl
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21
Q

Dopamine receptor agonists - MoA

A

Directly activate dopamine receptors in the stratum. Because they do not require functional dopaminergic neuron to produce their effects, they are sometimes helpful in advanced cases of PD, in which few dopaminergic neurons remain. They work by primarily activating D2 receptors and this leads to inhibition of the indirect neuronal pathway from the striatum to the thalamus and increase thalamic stimulation of the motor area of the cortex.

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22
Q

Dopamine receptor agonists - Adverse effects

A

Nausea
Orthostatic hypotension
Mental disturbances
Daytime sleepiness

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23
Q

Bromocriptine - MoA

A

Is a D2 agonist and a D1 antagonist.

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24
Q

Bromocriptine - Indication

A

Adjunct to levodopa in patients who have advanced PD and experience wearing off effects and on-off motor fluctuations.
Diabetes type 2

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25
Q

Bromocriptine - Adverse effects

A 
Decreased prolactin levels
Pulmonary and cardiac fibrosis
Orthostatic hypotension
Dry mouth
Nausea
Dose-related CNS effects: confusion, dyskinesias, sedation, vivid dreams and hallucinations
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26
Q

Pramipexole and Rotigotine - MoA

A

Selective D2 agonists

Also activates D3

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27
Q

Pramipexole - Indication

A

PD
Delay the need of levodopa
Restless leg syndrome

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28
Q

Pramipexole and Ropinirole - Adverse effects

A 
Dizziness 
Hallucinations
Insomnia
Nausea
Vomiting
Sedation
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29
Q

Pramipexole - Interaction

A

Cimetidine inhibits renal excretion and increases serum levels

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30
Q

Ropinirole - MoA

A

Selective D2 agonists

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31
Q

Ropinirole and Rotigotine - Indication

A

PD

Restless leg syndrome

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32
Q

Ropinirole - Interaction

A

Ciprofloxacin increases serum levels

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33
Q

Rotigotine - Adverse effects

A

Somnolence
Slight hypertension and tachycardia
Site irritation

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34
Q

Apomorphine - MoA

A

Does not bind to opioid receptors, but rather Dopamine agonist.

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35
Q

Apomorphine - Indication

A

Treatment of acute intermittent hypomobility (freezing) episodes associated with PD

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36
Q

Benztropine and Trihexyphenidyl - MoA

A

Antagonists at cholinergic muscarinic receptor and also exhibit antihistamine activity

Benztropine: may also inhibit the neuronal reuptake of dopamine and thereby prolong the action of dopamine

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37
Q

Benztropine and Trihexyphenidyl - Indication

A

May be helpful as adjunct therapy in combination with levodopa and other drugs that augment dopaminergic activity. They reduce tremor
Can also reduce parkinsonian symptoms caused by dopamine receptor antagonists, such as haloperidol

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38
Q

Benztropine and Trihexyphenidyl - Adverse effects

A 
Agitation
Confusion
Constipation
Delirium
Dry mouth
Memory loss
Urinary retention
Tachycardia
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39
Q

Benztropine and Trihexyphenidyl - Interactions

A

Additive anticholinergic effects with antihistamines and phenothiazines

40
Q

Drugs for Alzheimer disease

A 
Donepezil
Rivastigmine
Tacrine
Galantamine
Memantine
Caprylidene
Dextrometorphan
Quinidine
41
Q

Donepezil, Rivastigmine, Tacrine and Galantamine - MoA

A

Reversible acetylcholinesterase inhibitors.

Donepezil and Rivastigmine: improves cholinergic neurotransmission

42
Q

Donepezil - Adverse effects and Interactions

A

Bradycardia, diarrhea, GI bleeding, nausea, vomiting

Anticholinergic drugs inhibit effects

43
Q

Rivastigmine and Galantamine - Indication

A

Delays global cognitive impairment and slows the progression of AD.

44
Q

Rivastigmine and Galantamine - Advese effects

A

Risk of bradycardia and AV block

Nausea, vomiting, anorexia, weight loss

45
Q

Rivastigmine and Galantamine - Interactions

A

Both
Anticholinergic drugs inhibit effects.
Rivastigmine: Nicotine increases oral clearance
Galantamine: Inhibitors of CYP2D6 increase serum levels

46
Q

Tacrine - Adverse effects

A

Hepatotoxicity

Diarrhea, nausea, urinary incontinence

47
Q

Memantine - MoA

A

Noncompetitive antagonist at NMDA receptor. Blocks glutamate neurotransmission at NMDA receptors.

48
Q

Memantine - Indication

A

AD

Dementia

49
Q

Memantine - Adverse effects

A 
Confusion
Dizziness
Drowsiness
Headache
insomnia
50
Q

Caprylidene - MoA

A

Medical food that is metabolized into ketone bodies which the brain can use for energy when the processing of glucose is impaired.

51
Q

Caprylidene - Indication

A

Age associated memory impairment

AD

52
Q

Dextromethorphan

Quinidine - MoA

A

Dexmetromethorphan: inhibits excitatory glutamate release by agonist action at sigma-1 receptors and blocks NMDA receptors –> Excitatory neurotransmission that underlies emotion lability is reduced

53
Q

Dextromethorphan

Quinidine - Indication

A

Emotional lability (pseudobulbar effects). seen in pt w neurodegenerative diseases

54
Q

Dextromethorphan

Quinidine - Interactions

A

Quinidine is an inhibitor of CYP2D6 and therefore increases the bioavailability of dextromethorphan

55
Q

Drugs for Huntington Disease

A

Diazepam
Haloperidol
Tetrabenazine

56
Q

Diazepam - MoA

A

Potentiate GABA

57
Q

Diazepam - Adverse effects

A

Arrhytmias, CNS depression, drug dependence, hypotension, and mild respiratory depression

58
Q

Diazepam - Interactions

A

Alcohol and other CNS depressants potentiate effects.

Cimetidine increases and rifampin decreases serum level

59
Q

Haloperidol - MoA

A

Block dopamine receptors

60
Q

Haloperidol - Adverse effects

A

Extrapyramidal side effects

Increased prolactin levels

61
Q

Haloperidol - Interaction

A

Barbiturates and carbamazepine decrease and quinidine increases serum levels

62
Q

Tetrabenazine - MoA

A

Reversibly inhibit the human vesicular monoamine transporter type 2 VMAT2, resulting in decreased uptake of monoamine into synaptic vesicles and depletion on monoamine stores (dopamine, norepinephrine, serotonin) leading to decrease neurotransmitter release from nerve terminals.

63
Q

Tetrabenazine - Indication

A

Chorea in in HD

64
Q

Drugs for Multiple sclerosis

A 
Interferon beta-1b
Interferon beta-1a
Peginterferon beta-1a
Natalizumab
Daclizumab
Alemtuzumab
Mitoxantrone
Glatiramer acetate
Dalfampridine
Fingolimod
Teriflunomide
Dimethyl fumarate
Prednisone
Baclofen
65
Q

Interferon beta-1b - MoA

A

Increases the cytotoxicity of natural killer cells and increases the phagocytic activity of macrophages. In addition, it reduces the amount of interferon-gamma secreted by activated lymphocytes

66
Q

Interferon beta-1b - Adverse effects and interactions

A

Chills, diarrhea, fever, headache, hypertension, myalgia, pain and vomiting

Increases serum levels of zidovudine

67
Q

Natalizumab - MoA

A

Block the molecular pathway involving cell adhesion that draws lymphocytes into the CNS

68
Q

Daclizumab - MoA

A

Monoclonal antibody to IL-2 receptor, block interleukin-mediated activation of lymphocytes

69
Q

Alemtuzumab - MoA

A

CD52-directed cytolytic monoclonal antibody

70
Q

Alemtuzumab - Adverse effects

A

Life-threatening adverse effects of autoimmune, infusion reactions, and increased malignancies

71
Q

Mitoxantrone - MoA

A

Acts by suppressing the activity of T cells, B cells and macrophages that are thought to lead the attack on the myelin sheath. Antineoplastic drug

72
Q

Glatiramer acetate - MoA

A

Synthetic protein that mimics the structure of the myelin basic protein, a component of the myelin nerve fibers. This drug blocks myelin-damaging T cells by acting as a myelin decoy.

73
Q

Dalfampridine - MoA

A

Block potassium channels and enhance the conduction in damaged nerves

74
Q

Fingolimod - MoA

A

Sphingosine-1-phosphate receptor modulator, block the egress of lymphocytes from lymph nodes, reducing the number of lymphocytes in blood.

75
Q

Teriflunomide - MoA

A

Reduce the proliferation of overactive immune cells (including T- and B-cells) that attack and damage the nerve in the CNS by acting pyrimidine synthesis inhibitor.

76
Q

Teriflunomide- Adverse effects

A

Hepatotoxicity

77
Q

Dimethyl fumarate - MoA

A

Its main metabolite is monomethyl fumarate (MMF). MMF activates the Nuclear factor (erythroid-derived 2)-like 2 (Nfr2) pathway.

78
Q

Prednisone - Indication

A

Acute exacerbations of MS

79
Q

Prednisone - Adverse effects and Interactions

A

Aggrevation of: DM, GI-bleeding, mood changes, pancreatitis and seizures.

Barbiturates, Carbamazepine, phenytoin, rifampin decreases serum levels

80
Q

Which drugs are used for relapsing MS?

A 
Interferon beta-1a
Alemtuzumab
Fingolimod
Teriflunomide
Dimethyl fumarate
81
Q

Drugs for Amyotrophic lateral sclerosis

A

Baclofen
Gabapentin
Roluzole

82
Q

Baclofen - MoA + group

A

GABAb receptor agonist, when activated they reduce motor neuron excitability

Antispastic

83
Q

Baclofen - Adverse effects

A

Dizziness, Fatigue, Weakness

84
Q

Riluzole - MoA

A

Protect motor neurons from the neurotoxic effects of excitatory amino acids and prevent anoxia-related death of cortical neurons

May inhibit voltage-gates sodium channels that mediate the release of glutamate from neurons

85
Q

Riluzole - Indication

A

ALS
Prolongs the time before patients require a tracheotomy and also to prolong life by approximately 3 months.
More effective in those with bulbar-onset disease than in those with limb-onset disease

86
Q

Riluzole - Adverse effects and Interactions

A

Asthenia, diarrhea, dizziness, drowsiness, increased hepatic enzyme levels, nausea, vomiting, paresthesias, vertigo

Quinolones and Theophylline increases serum levels.
Omeprazole, rifampin and smoking decreases serum levels

87
Q

Antispastic Agents

A 
Baclofen
Cyclobenzaprine
Orphenadrine
Methocarbamol
Carisoprodol
Tizanidine
Dantrolene
Botulinum Toxin A
88
Q

Cyclobenzaprine

Orphenadrine - MoA and Indication

A

Centrally mediated effects on catecholamine reuptake, and antimuscarinic and antihistaminergic receptor actions

Muscle spasms by acute painful musculoskeletal conditions (short-term)-

89
Q

Methocarbamol - MoA

A

General CNS depression

90
Q

Carisoprodol - Indication

A

Muscle spasms caused by musculoskeletal conditions (short-term)

91
Q

Tizanidine - MoA and Indication

A

Centrally acting alpha2 adrenoceptor agonist, blocks nerve impulses through presynaptic inhibition of motor neurons.
Spasticity of MS

92
Q

Dantrolene - MoA

A

Block the release of calcium from the sarcoplasmic reticulum in muscle fibers, directly relaxes the muscle

93
Q

Dantrolene - Indication

A

Life saving in malignant hyperthermia triggered by halogenated anesthetics

Neuroleptic malignant syndrome
Spasticity

94
Q

Botulinum toxin A - MoA

A

Paralyses muscles by blocking the release of acetylcholine on the presynaptic side of the muscle endplate junction

95
Q

Botulinum toxin A - Indication

A 
Upper-limb spasticity in stroke patients
Cervical dystonia
Strabismus
Blepharospasm
Urinary incontinence resulting from detrusor overactivity in patients with spinal cord injury and MS
96
Q

Gabapentin - Group and Indication

A

Antiepileptic
ALS
Slows decline in muscle strength

97
Q

Gabapentin - Adverse effects and Interactions

A

Ataxia, dizziness, drowsiness, nystagmus, tremor

Antacids decreases serum levels

Pharmacology (55 decks)

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