Antiparkinsonism drugs

75問 • 1年前

問題一覧

Parkinsonism also know as

Idiopathic Parkinsonism, Primary Parkinsonism, Paralysis Agitans

Critical brain region (part of basal ganglia) for the production of dopamine and has a critical role in modulating motor movement and reward functions as part of the basal ganglia circuitry.

Substantia Nigra

Slowly progressive degenerative neurological disorder, characterized tremors, muscular rigidity, bradykinesia, and postural and gait abnormalities

Parkinsonism.

an eosinophilic rounded inclusion which is made up of alpha-synuclein is present in the affected substantia nigra. It appears in dopaminergic neurons before it dies. Aside from PD, it can also be found in other disease like DEMENTIA.

Lewy body

Sometimes it may have Genetic Predisposition. Mutation in?

PINK1, Parkin, alpha synuclein genes

its toxicity mainly by promoting the formation of reactive free radicals in the mitochondria of dopaminergic neurons in the substantia nigra. Results to destruction of dopaminergic neurons leading to Parkinson’s disease

MPP+ exhibits.

Because of inc Ach, most evident at rest and with low-frequency movement.

Tremor at rest

Muscle stiffness. It can affect any limb, but it's most common in the arms. It can affect one or both arms.

Muscle rigidity.

Difficulty in initiating movement

Akinesia

Slowness in performing common voluntary movements

Bradykinesia

Decrease body movement

Hypokinesia

Patient walk with a stopped, flexed posture

Gait & Postural difficulties

The cause is unknown while treatment may be palliative an the disease is incurable. Most patients suffer from this type of parkinsonism

Primary parkinsonism

⏤Minimal to no dopamine deficiency ⏤Mild to no improvement to dopaminergic drugs

Atypical Parkinsonsim

Type of Parkinson’s with a known cause: Disease, Poisoning, Infections or Drug intake

Secondary parkinsonism

Inhibit the uptake of dopamine in the vesicle. Increasing it’s degradation.

Reserpine

A rating tool used to gauge the the severity and progression of Parkinson's disease in patients It is used to evaluate the clinical efficacy of antiparkinson’s drugs and to monitor disease progression.

Unified parkinson's disease scale.

evaluation of mentation, behavior & mood

Part 1

Unilateral involvement (half of the body) includes major features of tremor, rigidity or bradykinesia, minimal functional impairment

Stage 1

Bilateral involvement (entire body) Same clinical manifestation to stage 1. Patient don’t have postural abnormalities

Stage 2

a self-reported evaluation of the activities of daily living (ADL)

Part 2

is a clinician-scored motor evaluation

Part 3

the Hoehn and Yahr staging of severity of Parkinson’s disease

Part 4

The Schwab and England ADL scale.

Part 5

Mild to moderate bilateral disease Mild postural imbalance, but still able to function independently

Stage 3

Bilateral involvement with postural abnormalities Patient requires substantial assistance

Stage 4

Severe disease Patient is restricted to bed or wheelchair unless aided.

Stage 5

Dopamine precursor

Levodopa

Drug of choice for Parkinsonism (not always used) ⏤ Most effective drug however prolonged use decreases its efficacy and increase adverse effects

Levodopa

L-dopa is converted to Dopamine by dopa decarboxylase thereby increasing the CNS levels of Dopamine in the brain. (T/F)

True

inhibit metabolism of L-dopa in the periphery thereby increase level of DA in the CNS

Carbidopa

DRUG HOLIDAYS discontinuance of the drug for 3–21 days temporarily improve responsivenes

Levodopa

more dopa is available for entry into the brain - Reduce the daily requirements of levodopa by approximately 75%

Carbidopa

What are drugs that may May increase efficacy of levodopa

Amantadine, benztropine, procyclidine, trihexyphenidyl

increase peripheral breakdown of L-dopa

Vitamin B6 pyridoxine

What are the ergot derivatives

Bromocriptine (Parlodel, Provasyn), Pergolide (Permax)

NON ERGOT DERIVATIVES

Apomorphine (Apokyn), Ropinirole (Requip), Pramipexole (Sifrol)

Dopamine 2 agonist

BROMOCRIPTINE, ROTIGOTINE, ROPINIROLE

Stimulates both D1 and D2 receptors

PERGOLIDE

preferential affinity for the D3 receptors

PRAMIPEXOLE

Also used in hyperprolactinemia but may increase risk of pulmonary fibrosis

Bromocriptine (Parlodel)

More effective than bromocriptine Also not used because it is associated with VHD (Valvular heart disease)

Pergolide (Permax)

Reduces symptoms of parkinsonism- smooths out fluctuations in levodopa response effective in on-off phenomenon

Pramipexole (Sifrol)

Monotherapy in px with mild dse and as a means of smoothing the response to L-dopa

An opioid derivative

Apomorphine (Apokyn)

First dose phenomenon

Bromocriptine

Cardiac valvulopathy

Pergolide

Inhibitors of Dopamine Metabolism

Mao inhibitors, COMT inhibitors

More potent (5x) than selegiline in preventing MPTP induced parkinsonism

Rasagiline

Retards the breakdown of dopamine Enhances and prolongs the antiparkinson’s effect of levodopa

Selegiline

Hepatic necrosis is associated with

Tolcapone

Rapid withdrawal causes hyperpyrexia and confusion

Entacapone

Prolong the action of levodopa by diminishing its peripheral metabolism Improves duration of “on-time” and dec “off-time”

Entacapone, Tolcapone

Dopamine Releaser

Amantadine symmetrel

It has been reported to antagonize the effects of adenosine at adenosine A2A receptors, which are receptors that may inhibit D2 receptor function.

Amantadine (Symmetrel)

A violaceous mottling of the skin with a "fishnet" reticular appearance.

Livedo reticularis

Blocks the excitatory neurotransmitter cholinergic influence in the basal ganglia

Anti muscarinic

What drug is used in Tremor & Rigidity Management

Anti muscarinic

Normal phenomenon, enhanced amplitude by anxiety, fatigue, thyrotoxicosis, IV Epinephrine

PHYSIOLOGIC POSTURAL TREMOR

A postural tremor, sometimes familial

Essential tremor

Present during movement

Intentional tremor

Due to parkinsonism

Rest tremor

Consist of rhythmic oscillatory movements around a join

Tremor

What are the drug odf choice in movement disorder

B-blockers, Metoprolol, Antiepileptic

Inherited disorder characterized by progressive chorea and dementia that begins at adulthood ⏤Related to imbalance of Dopamine, Ach, GABA, and perhaps other neurotransmitter in the basal ganglia

Huntington’s Disease

What isnthe drug of choice in Huntington’s Disease

Tetrabenazine, Reserpine

a condition of the nervous system. TS causes people to have “tics”.

Tourette Syndrome (TS)

What is the drug of choice in Tourette Syndrome (TS)

Haloperidol, Pimozide

⏤Uncontrollable urge to move the legs, usually because of an uncomfortable sensation.

Restless legs Syndrome

Restless legs syndrome what is the drug of choice

Dopaminergic, Ropinirole, Opioid analgesics and BZD

Inherited disorder of copper metabolism results in deposition of copper salts in the liver and other tissues

Wilson’s Disease

Wilson’s Disease in brain

Uncontrollable movement

Wilson’s Disease in eye

Kayser-Fleischer rings)

Wilson’s Disease in liver

Jaundice

Drug of choice in Wilson’s Disease

Chelating agent, Penicillamine

Cell structure.

Quinn Karylle Fuentes · 28問 · 2年前

Cell structure.