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General Terms to Learn:

Akathisia

An inner sense of
(motor restlessness)

restlessness

Central Serotonin Syndrome

Caused by over activation of central


5-HT receptors. Symptoms include
abdominal pain, diarrhea, sweating,
fever,
and
tachycardia.
Hypertension, delirium, myoclonus;
can induce cardiovascular shock and
death.

Delirium Tremors (DTs)

Autonomic instability, hallucinations,


tremor, hypertension, tachycardia,
and risk of seizures associated with
cessation of alcohol ingestion.

Dyskinesias

Abnormal involuntary movement

Extrapyramidal Syndrome (EPS)

Parkinson-like syndrome (Tremors


Rigidity
Akathisia,
Postrual
instability), akathisias, and dystonias
(Protruding of tongue)

Neuroleptic Malignant Syndrome

Characterized by muscular rigidity,


fever, and automatic instability;
associated
with
the
use
of
neuroleptic
medications
(eg,
haloperidol)

Tardive Dyskinesia (TD)

Syndrome of involuntary movements


typically involves mouth, face,
limbs., and trunk

Trigeminal Neuralgia

Sharp, stabbing pain that occurs in


one or more divisions of the
trigeminal nerve.

Wernicke-Korsakoff Syndrome

Neurologic
disorder
caused by
thiamine deficiency; often seen in
chronic alcoholic patients; symptoms
include
confusion,
ataxia,
and
memory impairment.

Drugs for Neurodegenerative Diseases


1. Parkinsons disease
2.Alzheimers disease
3.multiplesclerosis (MS)
4. amyotrophic lateral sclerosis (ALS)
Effect of drugs on the CNS:
1. Drugs may act presynaptically by influencing the production, storage,
release, or termination of action of neurotransmitters.
2. Agents may activate or block postsynaptic receptors.
* neurotransmissions in the cns is similar to that of the ans but the cns has
multiple synapse and lots of inhibitor and neurotransmitter unlike the ans
which only have the acetylcholine and the epinephrine, also the cns has
powerful inhibitory neurons that modulate the impulse transmissions.

PARKINSONS DISEASE
Parkinsonism is a progressive neurological disorder of muscle movement,
characterized by tremors, muscular rigidity, bradykinesia (slowness in
initiating and carrying out voluntary movements), and postural and gait
abnormalities. Most cases involve people over the age of 65, among whom
the incidence is about 1 in 100 individuals.
Etiology

The disease is correlated with destruction of dopaminergic neurons in the


substantia nigra with a consequent reduction of dopamine actions in the
corpus striatum, parts of the basal ganglia system that are involved in motor
control.

Secondary Parkinsonism
Drugs such as the phenothiazines and haloperidol, whose major
pharmacologic action is blockade of dopamine receptors in the brain,
may
produce
parkinsonian
symptoms
(also
called
pseudoparkinsonism).
Treatment
Many of the symptoms of parkinsonism reflect an imbalance between the
excitatory cholinergic neurons and the greatly diminished number of
inhibitory dopaminergic neurons. Therapy is aimed at restoring dopamine in
the basal ganglia and antagonizing the excitatory effect of cholinergic
neurons, thus reestablishing the correct dopamine/acetylcholine balance.
Drugs for Parkinsonism
1 Levodopa
2. Carbidopa
Adverse effect
- Anorexia
- Nausea
- Tachycardia
- Hypotension
- Psychiatric problem - Visual and auditory hallucinations
Interaction
o Pyridoxine
o Monamine Oxidase Inhibitor
Ex. Phenelzine
3. Selegiline (deprenyl)
-

MAO type B inibitor

Metabolize to amphetamine and methamphetamine

Rasagiline

4. Catechol-O-methyltransferase inhibitors
- 3-O-methyldopa
- Ex Entacapone, Tolcapone
- Albumin
- Cirrhosis
- Adverse effect fulminating hepatic necrosis
5. Dopamine receptor agonist
a. Bromocriptine
- hallucinations, confusion, delirium, nausea, and orthostatic
hypotension
- use in precaution in patient with myocardial infarction
- ergot derivative tend t lead to retroperitoneal fibrosis.
b. Apomorphine, pramipexole, ropinirole, and rotigotine
- pramipexole and ropinirole are oral form while apomorphine and
rotigotine are available for injection
- constipation
- interaction with cimetidine and flouxetine or other cytochrome P450
enzyme inhibitor
6. Amantadine
- used to treat influenza
- increasing the release ofdopamine, blocking cholinergic receptors,
and inhibiting the N-methyld- aspartate (NMDA) type of glutamate
receptors.
,
- restlessness,agitation, confusion, and hallucinations at high doses
may lead to toxic psychosis
- less potent than levodopa but less side effect
7. antimuscarinic agents
- benztropine, trihexyphenidyl, procyclidine, biperiden
- induce mood changes and produce xerostomia (dryness of the
mouth), constipation, and visual problems typical of muscarinic
blockers
- contraindicated with gastrointestinal peristalsis, glaucoma, prostatic
hyperplasia, or pyloric stenosis.
ALZHEIMERS DISEASE
- DEMENTIA

progressive loss of cholinergic neurons


and, presumably, cholinergic transmission within the
cortex
three distinguishing features
o 1) accumulation of senile plaques (-amyloid accumulations)
o 2) formation of numerous neurofibrillary tangles
o 3) loss of cortical neurons, particularly cholinergic neurons

It is postulated that inhibition of acetylcholinesterase (AChE) within


the CNS will improve cholinergic transmission, at least at those
neurons that are still functioning.
DRUGS FOR DEMENTIA
o ACETYLCHOLINESTERASE INHIBITOR
Mild to moderate alzheimer
donepezil, galantamine, and rivastigmine

tremors, bradycardia, nausea, diarrhea, anorexia and


myalgia
rivastigmine hydrolyzed by AChE to a carbamylate
metabolite and has no interactions with drugs that
alter the activity of CYP450 enzymes
o NMDA RECEPTOR ANTAGONIST
Stimulation of glutamate receptors in the CNS appears to
be critical for the formation of certain memories however
over stimulation( NMDA) may lead to excitotoxic or
programmed cell death or apoptotic
MEMANTINE
MODERATE TO SEVERE DEMENTIA

MULTIPLE SCLEROSIS
an autoimmune inflammatory demyelinating disease of the CNS
chronic, relapsing, or progressive disease that may span 10 to 20
years
DRUGS TO TREAT MS
A. Disease-modifying therapies
1. Interferon 1a and interferon 1b: The immunomodulatory
effects of interferonhelp to diminish the inflammatory responses
that lead to demyelination of the axon sheaths. Adverse effects of

these medications may include depression, local injection site


reactions, hepatic enzyme increases, and flulike symptoms.
2. Glatiramer: is a synthetic polypeptide that resembles myelin
protein and may act as a decoy to T-cell attack. Some patients
experience a postinjection reaction that includes flushing, chest
pain, anxiety, and itching. It is usually self-limiting.
3. Fingolimod: is an oral drug that alters lymphocyte migration,
resulting in fewer lymphocytes in the CNS. Fingolimod may cause
first-dose bradycardia and is associated with an increased risk of
infection and macular edema.
4. Teriflunomide: is an oral pyrimidine synthesis inhibitor that leads
to a lower concentration of active lymphocytes in the CNS.
Teriflunomide may cause elevated
liver enzymes. It should be avoided in pregnancy.
5. Dimethyl fumarate: is an oral agent that may alter the cellular
response to oxidative stress to reduce disease progression. Flushing
and abdominal pain are the most common adverse events.
6. Natalizumab: is a monoclonal antibody indicated for MS in
patients who have failed first-line therapies.
7. Mitoxantrone: is a cytotoxic anthracycline analog that kills T cells
and may also be used for MS.
B. Symptomatic treatment
spasticity,
constipation,
bladder
dysfunction,
and
depression
Dalfampridine, an oral potassium channelblocker, improves
walking speeds in patients with MS.
AMYOTROPHIC LATERAL SCLEROSIS
- ALS is characterized by progressive degeneration of motor neurons,
resulting in the inability to initiate or control muscle movement.
- Riluzole
o an NMDA receptor antagonist
o act by inhibiting glutamate release and blocking sodium
channels