Part 1 - Neuropharmacology Flashcards
What are the medications used for Parkinson’s Disease?
Levodopa, Carbidopa, (both increase dopamine)
Dopamine Agonists: Pergolide (PERMAX), Pramipexole (MIRAPEX)
MAO Inhibitors:
Selegiline (ELDEPRYL)
COMT Inhibitors:
Talcapone (TASMAR)
Entacapone (COMTAN)
Side effects of Levodopa? (Drug responsible for synthesis & degradation of dopamine)
GI, CV, Abnormal movements, psychiatric effects.
Drug incompatibilities and interactions.
- Pryidoxine
- Antipsychotic drugs
Side effects of Carbidopa (drug is a peripheral decarboxylase inhibitor; always used in combination with L-Dopa)
Does not penetrate the BBB
Decreases peripheral side effects of L-DOPA
Decreases required dose of L-DOPA
What are the 4 considerations of therapy in patients with PD?
“Wearing off” effect
“ON-OFF” phenomenon
“Drug Holidays” do not help
Depression needs treatment
What are the 2 direct Dopamine Agonists?
Pergolide (PERMAX), Pramipexole (MIRAPEX)
What are the central mechanisms of the 2 direct Dopamine Agonists?
Dopamine agonist - increases dopamine effects in basal ganglia
What are the side effects of the 2 direct Dopamine Agonists? (Drugs are used in combo with L-DOPA)
Ataxia, dystonia, akathesias, abnormal gait, hypertonia.
What do COMT and MAO Inhibitors do in general?
Synthesis and Degradation of Dopamine
What are the two common COMT Inhibitors?
Talcapone (TASMAR)
Entacapone (COMTAN)
What do COMT inhibiors do specifically?
Increases the duration action of L-DOPA
What are the adverse drug effects of COMT Inhibitors?
Abdominal pain, anorexia, confusion, lightheadedness, fever, hallucinations, INVOLUNTARY MUSCLE MOVEMENTS, severe diarrhea
What is the one common MAOI?
Selegiline (ELDEPRYL)
- Selective for MAO-B
- -Selective for Dopamine
What does MAOI do?
May slow the progression of the disease
What are the adverse drug effects of MAOIs?
Changes in behavior (mood swings, irritability, confusion, agitation)
Also: Dyskinesias, headache, palpitations
**Use with caution with anti-depressants, decongestants, stimulants
What are the 3 different Anticholinergics listed in the PPT?
Trihexyphenidyl (ARTANE)
Benztropine (COGENTIN)
Diphenhydramine (BENEDRYL)
*Avoid in the elderly - decreases acytelcholine instead of increasing dopamine.
Drugs that worsen PD and movement and older patients
Anti-psychotic drugs:
Haloperido (HALDOL) and chlorpromazine (THORAZINE)
Used for treatment of behavioral disorders
Actions - Central
Mechanism - Blockade of dopamine receptors
Effects - Parkinson-like, Tremor, Akithisia, akinesia.
Drugs that treat spasticity:
Baclofen, Botolinium toxin type A (BOTOX), Tizanidine (ZANAFLEX),
Drugs that are skeletal muscle relaxants:
Antispasmotics:
Chlorzoxazone (PARAFLEX, PARAFON FORTE), Cyclobenzaprine (FLEXORIL), DANTRALENE (DANTRIUM), Metaxalone (Skelaxin),
Anti-Histamines
Diphenhydramine (BENADRYL), Chlorpheniramine
Benzodiazepines (muscle inhibition)
Diazepam (VALIUM, others) Alprazolam (XANAX) Clonazepam (KLONOPIN) Lorazepam (ATIVAN) Midazolam (VERSED)
Anti-epileptic drugs
Valproic acid (DEPAKOTE), Phenytoin (DILANTIN), Carbamazepine (TEGRETOL)
Stimulants
Amphetamine (ADDERALL), methylphenidate (RITALIN)
Bupropion (WELLBUTRIN)?
Anticonvulsants
Phenytoin (DILANTIN) Carbamazepine (TEGRETOL) Valproic Acid (DEPAKOTE) Ethosuximide (ZARONTIN) Gabapentin (NEURONTIN) Lamotrigine (LAMICTAL)
Amphetamine, Methylphenidate
Release of norepinephrine, serotonin and dopamine
Increases attention, decreases impulsivity while producing stimulation in ADHD
NE reuptake inhibitor
Atomoxetine (STRATTERA)
ANTIPSYCHOTICS
1st generation (Typical)
Chlorpromazine (THORAZINE)
Thioridazine (MELLARIL)
Haloperidol (HALDOL)
2nd generation (Atypical) Clozapine (CLOZARIL) Risperidone (RISPERDAL) Quetiapine (SEROQUEL) Olanzepine (ZYPREXA)
Anti-depressants
Tricyclic Antidepressants (TCAs)
Nortriptyline (PAMELOR)
Amitriptyline (ELAVIL)
Desipramine (NORPRAMIN)
Selective Serotonin Reuptake Inhibitors (SSRIs) Fluoxetine (PROZAC) Paroxetine (PAXIL) Sertraline (ZOLOFT) Citalopram (CELEXA) Escitalopram (LEXAPRO) Fluvoxamine (Luvox)
Heterocyclics Venlafaxine (EFFEXOR) - SNRI Duloxetine (Cymbalta) Bupropion (WELLBUTRIN) Trazodone (DESYREL)
Herbals
St. John’s Wort
Monoamine Oxidase Inhibitors (MAOIs)
Tranylcypromine (PARNATE)
Anti-manic
Lithium (ESKALITH)
Carbamazepine (TEGRETOL)
Valproic Acid (DEPAKENE)
Lamotragine (LAMICTAL)
SSRIs
Fluoxetine (PROZAC), paroxetine (PAXIL), sertraline (ZOLOFT), fluvoxamine (LUVOX)
Drug that is potent in blocking reuptake of both norepinephrine and serotonin [SNRI]
Venlafaxine (Effexor)
Drug of choice in the treatment of manic/depressive disorder
Lithium
Anti-convulsants in mania
Valproate (DEPAKOTE)
First choice
Carbamazepine (TEGRETOL)
Lamotragine (LAMICTAL)
Gabapentin (NEURONTIN)
Sedative-Hypnotics
Barbiturates
Phenobarbital (LUMINAL)
Benzodiazepines Diazepam (VALIUM, others) Alprazolam (XANAX) Clonazepam (KLONOPIN) Lorazepam (ATIVAN) Midazolam (VERSED)
BZ1 Agonists
Zolpidem (AMBIEN)
Zaleplon (SONATA)
Eszopiclone (LUNESTA)
Buspirone (BUSPAR)
Non-benzodiazepine Benzodiazepine Receptor Agonists
Zolpidem (Ambien, Ambien CR)
Zaleplon (Sonata)
Eszopicone (Lunesta) – longer acting
Melatonin
Ramelteon (Rozerem)
MEDICATIONS THAT TREAT SEIZURES!
Anti-epileptic drugs: Valproic acid (DEPAKOTE), Phenytoin (DILANTIN), Carbamazepine (TEGRETOL)
Gabapentin (NEURONTIN) - used for seizure disorders
Lamotrigine (LAMICTAL) - Solo or adjunctive med for generalized or partial seizures, may be effective against absence seizures