CNS PHARMACO 3M

Amphetamines

stimulate the release of norepinephrine and dopamine from the brain and the sympathetic nervous system and inhibit the reuptake of these transmitters

Narcolepsy

characterized by falling asleep during normal waking activities

amphetamine sulfate

dextroamphetamine sulfate

lisdexamfetamine dimesylate

Combination: amphetamine and dextroamphetamine

amphetamine drug examples

alertness and euphoria

what can aphetamines cause?

amphetamine-like drugs

are generally more effective in treating ADHD than amphetamines (which are avoided)

Methylphenidate HCl

Dexmethylphenidate

Modafinil

examples of amphetamine like drugs

Amphetamine-like drugs

Increases child’s attention span and cognitive performance, and decreases impulsiveness, hyperactivity and restlessness

hypertensive crisis

Monoamine Oxidase Inhibitors (MAOIs)+ methylphenidate = ????

Analeptics

Act on the brainstem and medulla to stimulate respiration

dysrhythmia and seizure

Excess caffeine affects the CNS and heart = ???

pregnancy

Caffeine is contraindicated during ???

Anorexiants

Cause a stimulant effect on the hypothalamic and limbic regions of the brain to suppress appetite

weightloss

indication of anorexiants

Benzphetamine HCl �

Diethylpropion HCl

� Phentermine HCl

�Phentermine-topiramate

� Phendimetrazine

� Liraglutide

� Naltrexone HCl/ Buproprion HCl

�Setmelanotide

examples of anorexiants

Secobarbital sodium

Butabarbital sodium

Phenobarbital

Pentobarbital

Mephobarbital

SEDATIVE-HYPNOTICS examples

Ramelteon

the only major sedativehypnotic approved for long term use. This drug may be used to treat chronic insomnia

Phenobarbital

Long-acting barbiturates

BUTABARBITAL

Intermediate acting barbiturate

SECOBARBITAL , Pentobarbital

short acting barbiturate

furhter depression of CNS

alcohol, opioids, sedative- hypnotics + barbiturates =

hepatoxicity

Pentobarbital + acetaminophen

Alprazolam, Estazolam, Lorazepam, Temazepam, Triazolam, Quazepam, Diazepam, Flurazepam

examples of Benzodiazepines

Flumazenil

Antagonist of Benzodiazepines

anterograde amnesia

Adverse Reaction of Benzodiazepines

Zolpidem tartrate, Eszopiclone, Zaleplon

non-benzodiazepines example

before bedtime

when should non-benzodiazepines be taken?

Ramelteon

the newest category of sedative hypnotics

Phenytoin, fosphenytoin, carbamazepine, oxcarbazepine, valproic acid, topiramate, zonisamide and lamotrigine

suppressing sodium influx

Barbiturates, benzodiazepines, and tiagabine

Increasing the action of Gamma Aminobutyric Acid (GABA)

Valproic acid and ethosuximide

suppressing the calcium influx

Phenytoin/Hydantoins

Anti seizure drug that should not be used during pregnancy

Phenytoin/Hydantoins

effective for tonic-clonic seizure, partial seizures and status epilepticus

10-20 mcg/mL

therapeutic range of phenytoin

30 minutes to 2 hours

PO onset of pheyntoin

1\.5 to 3 hours

PO peak of phenytoin

6-12 hours

PO duration of phenytoin

wihthin minutes

IV onset of phenytoin

10-30 minutes

IV peak of phenytoin

up to 12 hours

IV duratuon of phenytoin

saline solution

phenytoin might be diluted with?

dextrose

phenyotin should not be with ???? to avoid drug precipiation

hyperglycemia

long period of hydantoin use leads to

urine may be a harmless pinkish red or reddish brown in color

this side effect can be seen in phenytoins

Phenobarbital

is prescribed to treat tonic-clonic, partial and myoclonic seizures as well as status epilepticus

Barbiturates/ Phenobabrital

15-40- mcg/mL

Succinimide

Used to treat absence seizure

Ethosuximide

example of succinimide

40- 100mcg/mL

Succinimide therapuetic range

Clonazepam

is effective for absence and myoclonic seizures but tolerance may occur 6 months after drug therapy starts

Clorazepate dipotassium

for partial seizures

Diazepam

administered through IV to treat status epilepticus

Iminostilbenes

used to control tonic-clonic and partial seizure

4-12 mcg/mL

Iminostilbenes/Carbamazapines therapeutic range

carbamazepine

� A potentially toxic interaction can occur when grapefruit juice is taken with ???

Valproate

for tonic-clonic, absence and partial seizure

50- 100mcg/mL

therpateutic range of Valproate

Phenytoin and carbamazepine

are linked to fetal anomalies (cardiac defects, cleft lip and palate

antiseizure drugs

tend to act as inhibitors of vitamin K

antiseizure drugs

can also increase the loss of folate in pregnant women

children younger than 2 yrs old

Valproic acid should not be given to ??

dopamine

an inhibitory neurotransmitter

released from dopaminergic neurons

maintains control of ACh and inhibits its excitatory response

Anticholinergics

Increase the effect of DA in the brain and by reducing the effect of Ach

inhibit the release of Ach

patients with glaucoma

contraindication of Anticholinergics

dry mouth �dry secretions, �urinary retention, �constipation, �blurred vision, �increase in heart rate

side effects of anticholinergics

low protein food

Administer levodopa-carbidopa with ???

dopamine agonists

stimulate dopamine receptors

Bromocriptine Mesylate

not as effective as carbidopa-levodopa in alleviating the symptoms

prolongs the action of levodopa

when MAO-B is inhibited.. the effect is that it

Selegiline HCl

can delay the use of carbidopa-levodopa by 1 year

May be ordered to patients newly diagnosed with PD

Tyramine

this should not be mixed with MAO-A in order to avoid hypertensive crisis

� Entacapone � Tolcapone

examples of Catechol-O-Methyltransferase Inhibitors

Tolcapone

1st COMT inhibitor given with levodopa for advanced PD

Entacapone

COMT inhibotor that doesnt affect liver function

urine can have brownish orange discoloration

harmless side effect in taking entacapone

levadopa concentration

COMT Inhibitor + Levodopa = ????

dopamine receptor antagonist

disrupts the activity of DA by blocking DA receptor sites without activating them

Istradefylline

�It reduces “off” periods

� It is a selective antagonist

� used as an adjuvant with levodopa-carbidopa therapy in adult PD patients who experience off episode

Amantadine

� acts on DA receptors

� exact mechanism in the treatment of PD is unknown

� may be taken alone or in combination with carbidopa-levodopa or anticholinergic

� produces improvement in symptoms of PD but tolerance develops � Also used for drug-induced parkinsonism

Pimavanserin

� classified as an atypical antipsychotic

� used to treat hallucinations and delusions associated with PD psychosis

Alzehimer’s disease

�is an incurable dementia illness

�characterized by a decline in a patient’s activities of daily living, cognitive abilities as well as changes in behavior.

\

Rivastigmine

� increases the amount of ACh at the cholinergic synapses

� tends to slow disease process

� AChE inhibitors increase cognitive functions for patients with mild to moderate Alzheimer Disease

� absorbed faster through GIT without food

� given twice a day

� contraindicated to patients with liver disease because hepatotoxicity may occur

Aducanumab

� an IV administered amyloid beta-directed antibody

� initiated in patients with mild cognitive impairment or mild dementia state of disease

� Reduces amyloid plaques in the brain by binding to forms of beta amyloid protein

Neostigmine

o must be given on time to prevent muscle weakness

o All other AChE drugs must be discontinued 8 hours before administration of neostigmine

o parenteral doses of neostigmine must be accompanied by intravenous atropine sulfate about 30 minutes before administering

Pyridostigmine

o half -life of oral pyridostigmine is 3 hours and is 1.5 hours for IV

o increases muscle strength

o Antidote: Atropine

Atropine

antidote for Pyridostigmine

myasthenic crisis

results from Inadequate dosing of pyridostigmine

cholinergic crisis

results from Overdosing of AChE inhibitors (30-60 mins after taking)

Prednisone is taken

If unresponsive to AChE Inhibitors:

Immunomodulators

are disease-modifying drugs

� the first line of treatment for MS

� can slow the progression of disease and prevent relapse

Glatiramer acetate

for relapsing form of MS

Alemtuzumab, ocrelizumab, and natalizumab

� a Monoclonal Antibody

� target and destroy certain cells while protecting the healthy cells

Diethyl fumarate

a selective immunosuppressant that can help delay disease progression

Mitoxantrone

a potent immunosuppressant used to reduce the relapse rate in patients with clinically worsening forms of MS

Cognitive

Disorganized thinking, memory difficulty, and decreased ability to focus attention.

Positive

exaggeration of normal function, incoherent speech, hallucinations, delusions, and paranoia

Negative

Decrease or loss in function and motivation

. ■ Tends to be more chronic and persistent.

Typical antipsychotic agents

● The conventional, or traditional group of antipsychotics

● First generation antipsychotics

● More helpful for managing positive symptoms

Atypical antipsychotic agents

● Second generation antipsychotics

● Newest treatment for both positive and negative symptoms of schizophre

� aliphatic � piperazine � piperidine

Phenothiazines

� butyrophenones � dibenzoxazepines � dihydroindolones � thioxanthenes

Non-phenothiazines