Mechanisms of action, seizures, sedative hypnotics, dopamine precursors antagonist , inhibitors and misc drugs

Sodium Channel Blockers

Phenytoin, Carbamazepine, Oxcarbazepine, Lamotrigine, Topiramate

drugs that enhance GABA

Benzodiazepines, Phenobarbital, Tiagabine, Gabapentin, Vigabatrin

T type calcium channel blockers

Ethosuximide

Glutamate Receptor Antagonists

Felbamate, Topiramate

Idiopathic Mechanisms

Levetiracetam

What Partial (Focal) Seizure and drugs of choice

begins in a specific area of the brain and can either remain localized or spread to other areas.

Carbamazepine, Oxcarbazepine, Lamotrigine

Generalized tonic clonic seizure drug of choice

Valproate, Lamotrigine, Levetiracetam

Drugs of choice for absence seizures

Ethosuximide, Valproate

Drugs of choices for myoclonic atonic seizures

Valproate, Lamotrigine, Levetiracetam

Alternatives for focal seizures

Valproate, Topiramate, Phenytoin

Alternative for generalized tonic clonic

Topiramate, Zonisamide, Phenytoin

Alternative for absence seizures

Lamotrigine, Clonazepam

Alternatives for myoclonic atomic seizures

Topiramate, Zonisamide, Clonazepam

Examoles of benzodiazepines

Diazepam (Valium)

Lorazepam A(viatn) -

Midazolam (Versed)

Chlordiazepoxide

Midazolam (Versed)

Triazolam (Halcion)

Alprazolam (Xanax)

Clonazepam (Klonopin)

Flurazepam (Dalmane)

Temazepam (Restoril)

Mechanism of action of benzodiazepines

Enhance GABA activity • Increases eht frequency of

the openig of GABA activated C-l channels

(causes hyperpolarization)

Uses of benzodiazepines

Anxiety

I n s o m n i a Seizure management (Anticonvulsant)

Insomia

Alcohol withdrawal

Adverse effects

Sedation Tolerance

Withdrawal symptoms Daytime Sedation Respiratory depressio

Barbiturates (rarely used)

(-al)

Phenobarbital

Thiopental

MOA of barbiturates

Potentiate GABA effects

Bind to GABA receptor C-I Channel complex and mimic GABA

Uses of barbs

Anesthesia induction

Seizure control

Adverse effects of barbs

Respiratory depression,

high addiction potential

CNS depression

- Tolerance Physical dependance

Narrow TI

Z drugs

Zolpidem, Eszopicione

MOA of z drugs

Selectively act on GABA-A receptors

Uses of z drugs

Insomnia

Adverse effects of z drugs

Sleepwalking, dizziness, dependency

Melatonin Agonists

Ramelteon

Mechanisms of action of Melatonin Agonists

Agonist at melatonin - receptors (MT1, MT2)

Therapeutic uses of melatonin receptors

Sleep onset insomnia

Adverse effects of melatonin agonist

Minimal affects

Orexin Antagonists

Suvorexant

MOA OF Orexin Antagonist

Inhibit orexin receptors

Uses for Orexin Antagonist

Insomnia

Affects of Orexin Antagonist

Daytime drowsiness, potential for dependency

Midazolam

Versed

Short acting 2-3 hours half life

Triazolam

Hallcom

Short acting 2-3 hour half life

Aprazolam

Xanax

Intermediate acting

12-15 hour half life

Estazolam

Prosom

Intermediate

10-24

Lorazepam (Ativan)

Intermediate

10-20

Temazepam (Restoril)

Intermediate

10-40

Clonazepam (Klonipin)

Long acting

18-50

Clorazepate (Tranxene)

Long acting

40-50

Diazepam

Valium

Long acting

20-80

Flurazepam

Dalmane

Long acting

40-100

Drug used for Preanesthetic, intraoperative uses

Midazolam

Drugs used for insomnia

Trizolam

Flurazepam

Drugs used for Anxiolytic, agoraphobia

Aprazolam and Lorazepam

name a anxiolytic anticonvulsant

Clorazepate

Name a drug used for anticonvulsant

Clonazepam

Name the drug used for Anxiolytic, status epilepticus, muscle relaxant, anesthetic premed

Diazepam

What is Parkinson’s

achronic, progressive neurologic disease caused by dopaminergic neuron loss

drugs used to help Parkinson’s restore

dopamine levels in the basal ganglia and counterbalance acetylcholine activity.

Dopamine precursors

Levodopa

Carbidopa

Sinemet

Levodopa MOA and uses

Converted to dopamine in the brain.

Used for symptoms of Parkinson’s

Adverse effects of levodopa

Nausea, vomiting, orthostatic hypotension, dyskniesais, on-of phenomenon, cardiac dysrhythmias.

GABA Activity

The activity related to gamma-aminobutyric acid, an inhibitory neurotransmitter that helps regulate neuronal excitability.

Adverse effects of carbdipoa

Reduces peripheral side effects of levodopa.

MOA and use for Sinemet

Combination of levodopa and carbidopa.

Gold standard therapy.

Adverse effects of sinemet

Combination reduces levodopa- related peripheral side effects but does not eliminate central side effects.

Dopamine agonist drugs

Apomorphine

Pramipexole

Ropinirole

BromocripCne

MAO B inhibitor drugs

Selegiline

Rasagiline

COMT inhibitors

Entacapone

Tolcapone

Stalevo

Apomorphine

Stimulates dopamine receptors; used during "off” episodes.

Apomorphine therapeutic use

Rescue therapy for on off phenomenon

Adverse Effects of Apomorphine

Severe nausea, postural hypotension, dizziness, somnolence.

Pramipexole

Binds to and acIvates dopamine receptors.

Therapeutic action for pramipexole

Early PD and adjunct in advanced PD

Adverse effects of pramipexole

Nausea, dizziness, sleep abacks, impulse control disorders.

Ropinirole

Stimulates dopamine receptors

Therapeutic use of Ropinirole

Early PD or adjunct to levodopa.

Adverse effects of ropinrole

Similar to pramipexole: dizziness, postural hypotension, compulsive behaviors.

BromocripCne

Ergot-derived agonist; also sImulates serotonin receptors.

Therapeutic use of bromocriptine

Rarely used due to side effects.

Adverse effects of BromocripCne

Nausea, fibrosis, hallucinaIons.

Selegiline

Inhibits MAO-B, decreasing dopamine breakdown.

Therapeutic use

Mild PD, adjunct to levodopa.

Selegine adverse effects

Insomnia, nausea, headache, potenIal interacIon with tyramine-containing foods.

Rasagiline

Irreversible MAO-B inhibitor; neuroprotecIve effects.

Therapeutic use of ragagrille

Mild PD or as levodopa adjunct.

Adverse reactions of selegille

Similar to selegiline, with less pronounced side effects.

Entacapone

Inhibits COMT, prolonging the effect of levodopa.

Therapeutic use of entacapone

Adjunct to levodopa in advanced PD.

Adverse effects of entacaphone

Diarrhea, orange urine discoloraIon, hepatotoxicity (rare).

Tolcapone

Similar to entacapone but more potent.

Therapeutic use of tolcapone

Used only when entacapone fails.

Adverse effects of cocaine

Higher risk of hepatotoxicity; requires liver enzyme monitoring.

Stalevo

CombinaIon of levodopa, carbidopa, and entacapone.

Stalevo Therapeutic use

Advanced PD

Adverse effects of stalevo

Combines side effects of all components; enhances levodopa’s efficacy.

Miscellaneous PD Drugs

Amantadine

Anticholinergics

Amantadine

Enhances dopamine release; blocks NMDA receptors.

Amantadine therapeutic use

Early-stage PD or levodopa dyskinesias.

Adverse effects of amantide

CNS effects (e.g., confusion, hallucinaIons), GI upset, livedo reIcularis (mobled skin discoloraIon).

AnCcholinergics

Block acetylcholine acIvity in basal ganglia.

Therapeutic use of AnCcholinergics

Tremor-dominant PD.

Therapeutic use of AnCcholinergics

Dry mouth, blurred vision, consIpaIon, urinary retenIon, cogniIve impairment.

Levopoda/carbidopa

Most effecIve for PD Moderate efficacy. symptoms.

Dopamine agonist

Moderate efficacy.

MAO B Inhibitors

Mild efficacy.

COMT INHIBITORS

Enhances levodopa’s efficacy.