NERVOUS SYSTEM I FINAL EXAM DRUGS

1ST GENERATION ANTIPSYCHOTIC

THORAZINE

1ST GENERATION ANTIPSYCHOTIC

SERENTIL

1ST GENERATION ANTIPSYCHOTIC

MELLARIL

1ST GENERATION ANTIPSYCHOTIC

PROLIXIN

1ST GENERATION ANTIPSYCHOTIC

TRILAFON

1ST GENERATION ANTIPSYCHOTIC

STELAZINE

1ST GENERATION ANTIPSYCHOTIC

NAVANE

1ST GENERATION ANTIPSYCHOTIC

HALDOL

1ST GENERATION ANTIPSYCHOTIC ACCORDING TO SYLLABUS AND LEXICOMP, BUT 2ND GEN ACCORDING TO MONIRI AND BY LOOKING AT THE STRUCTURE

LOXITANE

1ST GENERATION ANTIPSYCHOTIC

MOBAN

2ND GENERATION ANTIPSYCHOTIC

CLOZARIL

2ND GENERATION ANTIPSYCHOTIC

RISPERDAL

2ND GENERATION ANTIPSYCHOTIC

ZYPREXA

2ND GENERATION ANTIPSYCHOTIC

SEROQUEL

2ND GENERATION ANTIPSYCHOTIC

GEODON

2ND GENERATION ANTIPSYCHOTIC

ABILIFY

2ND GENERATION ANTIPSYCHOTIC

INVEGA

2ND GENERATION ANTIPSYCHOTIC

FANAPT

2ND GENERATION ANTIPSYCHOTIC

SAPHRIS

HYDANTOIN ANTIEPILEPTIC

DILANTIN

BARBITURATE ANTIEPILEPTIC

LUMINAL

ANTIEPILEPTIC

• NA+ CHANNEL BLOCKER
• METABOLIZED INTO PHENOBARBITAL, WHICH IS THEN ALSO ANTIEPILEPTIC BY MANY MORE MECHANISM AS WELL

MYSOLINE

IMINOSTILBENE ANTIEPILEPTIC

TEGRETOL

IMINOSTILBENE ANTIEPILEPTIC

TRILEPTAL

SUCCINIMIDE ANTIEPILEPTIC

CA+ CHANNEL BLOCKER, WHICH IS GOOD FOR ABSENCE SEIZURES

ZARONTIN

ANTIEPILEPTIC OR BIPOLAR THERAPY

NA+ AND CA+ CHANNEL BLOCKER

DEPAKENE

BENZODIAZEPINE ANTIEPILEPTIC

KLONOPIN

BENZODIAZEPINE ANTIEPILEPTIC

VALIUM

BENZODIAZEPINE ANTIEPILEPTIC

NO CYP METABOLISM, STRAIGHT TO GLUCURONIDATION

ATIVAN

ANTIEPILEPTIC

NEURONTIN

ANTIEPILEPTIC

LAMICTAL

ANTIEPILEPTIC

KEPPRA

ANTIEPILEPTIC

GABITRIL

ANTIEPILEPTIC

TOPAMAX

ANTIEPILEPTIC

FELBATOL

ANTIEPILEPTIC

ZONEGRAN

ANTIEPILEPTIC

VIMPAT

DOPAMINE PRECURSOR FOR PARKINSON'S

NOT HIGHLY USEFUL BY ITSELF. CAUSES PERIPHERAL SIDE EFFECTS, AND NOT MUCH CAN CROSS THE BBB WITHOUT BEING METABOLIZED FIRST BY EITHER COMT OR DOPA DECARBOXYLASE (AAD). L-DOPA MUST CROSS THE BBB BEFORE BEING COVERTED TO DOPAMINE SINCE DOPAMINE CANNOT CROSS THE BBB. AFTER BBB CROSSING AND CONVERSION TO DOPAMINE IT CAN STIMULATE MOVEMENT IN THE NIGROSTRIATAL PATHWAY.

DOPAMINE PRECURSOR COMBO THERAPY FOR PARKINSON'S

L-DOPA IS A PRECURSOR TO DOPAMINE, BUT L-DOPA IS ABLE TO CROSS THE BBB WHEN ADMINISTERED (BUT ONLY IN SMALL AMOUNTS BY ITSELF, AND WITH PERIPHERAL SIDE EFFECTS)

CARBIDOPA IS A DOPA DECARBOXYLASE INHIBITOR THAT BINDS VITAMIN B6 (PYRIDOXINE). VIT B6 IS A NECESSARY COFACTOR TO DOPA DECARBOXYLASE, SO IT NOW CANNOT METABOLIZE L-DOPA TO DOPAMINE IN THE PERIPHERY. REMEMBER ONLY L-DOPA CAN CROSS THE BBB, SO IT MUST STAY L-DOPA UNTIL AFTER BBB CROSSING, AND THEN BE CONVERTED FOR USE IN THE NIGROSTRIATAL PATHWAY.

SINEMET

DOPA DECARBOXYLASE (AAD) INHIBITOR ADJUNCT THERAPY FOR PARKINSON'S

ALLOWS MORE L-DOPA TO CROSS THE BBB, EVEN IN LOWER DOSES, WHICH LOWERS PERIPHERAL SIDE EFFECTS AND STIMULATES MORE MOVEMENT IN THE NIGROSTRIATAL PATHWAY

LODOSYN

DOPAMINE PRECURSOR COMBO THERAPY FOR PARKINSON'S

L-DOPA CROSSES THE BBB TO BE CONVERTED TO DOPAMINE BY DOPA DECARBOXYLASE (AAD) AND STIMULATE MORE MOVEMENT IN THE NIGROSTRIATAL PATHWAY (ALONE IT IS NOT VERY USEFUL AND SOMEWHAT TOXIC)

CARBIDOPA IS A DOPA DECARBOXYLASE (AAD) INHIBITOR IN THE PERIPHERY ONLY (WHICH LOWERS PERIPHERAL SIDE EFFECTS AND ALLOWS L-DOPA TO CROSS THE BBB IN GREATER AMOUNTS TO BE CONVERTED TO DOPAMINE FOR THE NIGROSTRIATAL PATHWAY WHERE IT'S NEEDED

ENTACAPONE IS A COMT INHIBITOR IN THE PERIPHERY ONLY, SO MORE L-DOPA IS ABLE TO CROSS THE BBB AS NEEDED

STALEVO

• MONOAMINE OXIDASE INHIBITOR
• FOR PARKINSON'S OR DEPRESSION

DOES NOT TEND TO CONTRIBUTE TO HYPERTENSIVE CRISIS AS IT DOES NOT INHIBIT MAO-A IN THE GUT

ELDEPRYL, EMSAM(PATCH)

MAOI USED FOR PARKINSON'S

LOWERS DOPAMINE CONVERSION TO DOPAC BY MAO-B IN THE BRAIN. THIS LOWERS POTENTIAL FREE RADICAL DAMGE TO SUBSTANTIA NIGRAL DOPAMINERGIC NEURONS, AND SLOWS PROGRESSION OF PARKINS'S DISEASE

AZILECT

COMT INHIBITOR FOR PARKINSON'S

• PERIPHERY AND BRAIN
• AIDS PROPER USE OF L-DOPA
• HIGHLY TOXIC AND ONLY A LAST RESORT

TASMAR

COMT INHIBITOR FOR PARKINSON'S

PERIPHERY ONLY, BUT INCREASES AMOUNT OF L-DOPA THAT MAKES IT THROUGH THE BBB TO BE CONVERTED TO DOPAMINE AND UTILIZED TO ADD MOVEMENT IN THE NIGROSTRIATAL PATHWAY

COMTAN

D2 FAMILY RECEPTOR AGONIST FOR PARKINSON'S

NEUPRO

D2 FAMILY RECEPTOR AGONIST FOR PARKINSON'S

PARLODEL

D2 FAMILY RECEPTOR AGONIST FOR PARKINSON'S

MIRAPEX

D2 FAMILY RECEPTOR AGONIST FOR PARKINSON'S

REQUIP

• DA RECEPTOR AGONIST FOR PARKINSON'S
• PRIMARILY AN ANTIVIRAL

WAS THE MODEL USED TO DEVELOP MEMANTINE

SYMMETREL

• MUSCARINIC RECEPTOR ANTAGONIST
• FOR PARKINSON'S

COGENTIN

• MUSCARINIC RECEPTOR ANTAGONIST
• FOR PARKINSON'S

BENADRYL

• MUSCARINIC RECEPTOR ANTAGONIST
• FOR PARKINSON'S

ARTANE

• ANTICHOLINESTERASE AGENT
• FOR ALZHEIMER'S

COGNEX

• ANTICHOLINESTERASE AGENT
• FOR ALZHEIMER'S

ARICEPT

• COVALENT ANTICHOLINESTERASE AGENT
• FOR ALZHEIMER'S

EXELON (PATCH)

• ANTICHOLINESTERASE AGENT
• FOR ALZHEIMER'S

RAZADYNE

• NMDA RECEPTOR ANTAGONIST
• FOR ALZHEIMER'S

NAMENDA

MEDICAL FOOD FOR ALZHEIMER'S

INCREASES KETONE BODIES IN THE BLOOD, WHICH INCREASES THE BRAIN'S BLOOD GLUCOSE UTILIZATION

AXONA

FOR HUNTINGTON'S DISEASE (A HYPERKINETIC DISORDER IN EARLY STAGES)

MOA: WANT TO REDUCE MOVEMENT

1: INHIBIT VMAT2 - LOWER DA PRODUCTION

2: BLOCK POST-SYNAPTIC STRIATAL D1 AND D2 RECEPTORS (SINCE DA ATTACHES TO EITHER OF THESE TO CREATE MOVEMENT IN NIGROSTRIATAL PATH)

• SIDE EFFECT:
• -INHIBITING VMAT LEADS TO LOWERED PRODUCTION OF DA, NE, EPI, 5HT, H

• LOWERED NE, EPI MEANS HYPOTENSION
• LOWERED H MEANS DROWSINESS
• LOWERED 5HT MEANS DEPRESSION
• LOWERED DA COULD MEAN EPS (PARKINSON'S LIKE SIDE EFFECTS)

XENAZINE

• FOR AMYOTROPHIC LATERAL SCLEROSIS
• (LOU GEHRIG'S DISEASE)

MOA: LOWER GLUTAMATE TRANSMISSION

• -BLOCKS VOLTAGE NA+ CHANNELS
• -INHIBITS POST-SYNAPTIC GLUTAMATERGIC NMDA AND KAINATE Rs
• -INCREASES ACTIVITY/EFFICIENCY OF GLUTAMATE REUPTAKE TRANSPORTERS

DOES NOT AFFECT AMPA RECEPTORS

METABOLIZED BY CYP 1A2 AND THEN GLUCURONIDATION

CAN ELEVATE TRANSAMINASES, WHICH REQUIRES LIVER FUNCTION LAB TESTS

RILOTEK

• SYMPTOMATIC TREATMENT OF SPASTICITY
• (RESISTANCE TO MOVING A LIMB AT A JOINT, BUT FOLLOWED BY RELAXATION)

MOA:

-GABA-B (Gi COUPLED) AGONIST THAT WORKS PRIMARILY TO INHIBIT SPINAL CORD INTERNEURONS THAT ARE INVOLVED IN SYNAPTIC REFLEXES

REMEMBER THAT BENZODIAEPINES WORK ON GABA-A RECEPTORS TO ESSENTIALLY GET THIS SAME RESULT, AMONGST OTHER THINGS

FOR MULTIPLE SCLEROSIS

COPAXONE

FOR MULTIPLE SCLEROSIS

AVONEX, REBIF, BETASERON

FOR MULTIPLE SCLEROSIS

TYSABRI

FOR MULTIPLE SCLEROSIS

NOVANTRONE

CNS STIMULANT FOR NARCOLEPSY

PROVIGIL

CNS STIMULANT FOR NARCOLEPSY/ADHD

ADDERALL, DEXEDRINE, DEXTROSTAT

CNS STIMULANT USED TO TREAT NARCOLEPSY

DESOXYN

CNS STIMULANT FOR NARCOLEPSY

RITALIN,

NARCOLEPSY

NARCOLEPSY

NARCOLEPSY

• CNS DEPRESSANT FOR NARCOLEPSY
• (SLEEP AID)

XYREM

ETHANOL CONSUMPTION PREVENTATIVE

ANTABUSE

ETHANOL CONSUMPTION PREVENTATIVE

CAMPRAL

ETHANOL CONSUMPTION PREVENTATIVE

REVIA, DEPADE

SMOKING CESSATION AGENT

ZYBAN

SMOKING CESSATION AID

CHANTIX

CANNABINOID RECEPTOR(CB1) AGONIST

ANTIEMETIC

CESAMET

CANNABINOID RECEPTOR(CB1) AGONIST

ANTIEMETIC

DRONABINOL

CANNABINOID 1 & 2 RECEPTOR AGONIST

ANALGESIC AND ANTIEMETIC

SATIVEX

CANNABINOID RECEPTOR ANTAGONIST

RIMONABANT

SUBSTRATE ANTICHOLINESTERASE

REVERSIBLE, AND CARBAMYLATES ACH-ESTERASE

100X AFFINITY OF ACH

CLASSICAL PROTOTYPE OF ANTICHOLINESTERASES

ESERINE, ANTILIRIUM

SUBSTRATE ANTICHOLINESTERASE

CARBAMYLATES ACH-ESTERASE

VIRTUALLY IRREVERSIBLE

PROTONATED QUATERNARY AMMONIUM SALT DOES NOT ALLOW BBBX, SO NOT GOOD FOR PARKINSON'S, ONLY MYASTHENIAS GRAVIS

REGENOL, MESTINON

REVERSIBLE ANTICHOLINESTERASE

LACKS CARBAMATE MOEITY

PHTHALAMIDE DERIVITIVE, PHTHALAMIDE GROUP INTERACTS WITH HYDROPHOBIC BINDING SITE 2 ON ACH-ESTERASE

DOES NOT HAVE ACTIVITY WITH THE ESTERATIC SITE ON ACH-ESTERASE

OCH3 E-WITHDRAWING GROUP ADDS ACH-ESTERASE AFFINITY

PIPERADINE BINDS ANIONIC SITE

SATURATION OF AROMATIC RINGS WOULD LEAD TO LESS PI PI STACKING AND DECREASED ACTIVITY

BENZENE RING BINDS HYDROPHOBIC BINDING SITE 1 ON ACH-ESTERASE