Pharmacology Exam 2 Wiggins

LSD type hallucinogens

class, MOA

class 1 drug; MOA unknown but suggests 5HT2A receptors with agonism and antagonism

how long do LSD type hallucinogens last? When is their peak?

usually last 12 hour

peak around 1-2 hrs

lysergic acid diethylamide

associated with flashbacks

when was LSD discovered and was did it formerly treat?

1938 used to treat alcoholism and mental illnesses but there are no current therapeutic uses

Other types of LSD-type hallucinogenics

tryptamine derivatives (psilocybin and DMT)

phenylethylamine derivates (mescaline and DOM)

tryptamine derivative and 2 examples

LSD Type drugs Ex) psilocybin and DMT

phenylethylamine derivative and 2 examples

LSD Type Ex) mescaline and DOM

Effects of LSD Type Drugs

synesthesia (mix up senses)

potent stimulant

Psychomotor Stimulants

drugs such as amphetamine and cocaine that produce their effect by stimulating the effects of certain neurotransmitters, specifically norepinephrine, dopamine, and serotonin

designer drugs

synthetic drugs that are made to imitate the effects of other drugs

examples of designer drugs

amphetamines, cocaine, MDA, MDMA, and pure crystal MDMA

Amphetamines

type of drug, NT, some facts

psychomotor stimulant

increase NE and DA

DA causes euphoria

discontinues use = profound sleep followed by crash (depressed and disagreeable)

psychosis similar to paranoid schizophrenia

Cocaine originated

in 1855 South American Natives chewed the cocoa leaves to ward of fatigue, hunger, and altitude sickness

cocaine is a ____ drug because until ____ it was used to treat everything, which makes it a class ___ drug

wonder drug because until 1914 it was used to treat everything, which makes it a class 2 drug after having some medical uses

can you smoke cocaine? what can you do it make it into crystal crack

cannot smoke cocaine, can ALKALINIZE it to make it into crystal crack

Phencyclidine (name, what it is orig used for)

PCP "angel dust" ; drug originally developed as a surgical anesthetic that was discontinued due to adverse patients reactions (delirium)

what is still used in vets for primate immobilization

Phencyclidine, PCP, angel dust

MOA for Phencyclidine or PCP

glutamate (excitatory NT) antagonist, especially NMDA (memory/glutamate) receptor

what does PCP do to you

disorders of body image, common to have elongation or shrinkage in perception of extremities

- slowed reflexes, ataxia, depressive state, paranoid

- quick tolerance

marijuana class?

class 2 because medical uses

hashish

extracted sticky resin from marijuana

what are the effects of marijuana due to?

cannabinoids (THC) has psychoactive properties

MOA of marijuana

not completely understood, binds to cannabinoid receptors which are important in learning and memory so these are impaired

effects or marijuana

euphoria, increased sociability, conversations focus on present time, time passes slowly, short-term memory impaired

chronic use of marijuana can cause

psychosis, anxiety, dysphoria, decreased sperm count, sporadic ovulation

THC has been investigated to treat (3 things)

nausea, vomiting, pain

Dronabinol is a ___ analog and is approved to _____

Dronabinol is a THC analog that is approved to stimulate appetite for patients with AIDS

Antieplieptic Drugs

drugs that treat seizures, epilepsy, convulsions

seizure definition

abnormal electrical discharge of brain neurons

general epilepsy

involves both the left and right hemispheres of the brain, there are three kinds: tonic-clonic (grand mal), atonic, and absence (petit mal)

partial epilepsy

seizures are localized to specific areas of the brain but can become generalized. there are two type: simple partial, and complex partial

effective drugs for seizures (2)

anticonvulsants which are given by IM or IV and antiepileptics which decreases brain excitability

Barbiturates MOA

bind to receptors on Cl- channel to enhance GABA (inhibitor) effects, this decreases the glutamate (excitability) response

phenobarbital

AC/AE/both?

Class of drug?

anticonvulsant (AC) and antiepileptic (AE)

is from class of barbiturates

what is the safest and most used drug to treat seizures in infants

phenobarbital

Phenytoin trade name

Dilantin

Phenytoin

AC/AE/both?

MOA

Phenytoin = Dilantin

potent antiepileptic

MOA: Prolongs Na+ channel inactivation, decreasing rapid firing, also increases GABA (inhibitor NT) , and decreases release of glutamate (excitatory NT)

Phenytoin (Dilantin) is what class of drugs?

Hydantoins

Carbamazepine trade name

Tegretol

carbamazepine is indicated for what

most types of seizures, mania, and bipolar disorder

what can treat trigeminal neuralgia and why

carbamazepine (tegretol) can treat because of its analgesic properties

How does carbamazepine work?

blocks Na+ channels to prolong inactivation which decreases rapid firing. increases release of GABA and decreases release of glutamate

side effects or carbamazepine (tegretol)

N&V, drowsiness, dizziness. more serious include jaundice, liver issues, and bone marrow depression which can lead to aplastic anemia. associated with spina bifida and developmental delay

trade name of Valproic acid

Depakene

what does valproic acid (depakene) treat

valproic acid (depakene) treats all types of epilepsy

what is the MOA of valproic acid (depakene)

block Na channels to prolong inactivates, blocks glutamate NMDA receptors (excitatory), and increases GABA (inhibitor) effects with little sedation

side effects of valproic acid (depakene)

N&V, diarrhea, and tremors. potentially fatal liver toxicity which is prevalent in young patients, and birth defects like spina bifida

Primidone trade name

Mysoline

primidone (mysoline) is chemically related to what and metabolized into what

barbiturates and metabolized into phenobarbital which is used to treat epilepsy in infants

trade name of Levetiracetam

keppra

levatiracetam (keppra) MOA

poorly understood but may affect GABA and glutamate activity.

levatiracetam (keppra) is indicated for what

levatiracetam (keppra) is indicated as adjunctive treatment of partial seizures

topiramate trade trade

topiramate trade name is topamax

MOA for Topiramate (Topamax)

is not clearly understood but may interfere with NA channels and increase GABA effects

what it Topiramate (Topamax) indicated for

Topiramate (Topamax) is indicated for tonic-clonic (grand mal) and partial seizures

trade name for Zonisamide

Zonisamide trade name is (Zonegram)

MOA for Zonisamide (Zonegran)

interferes with Na and Ca ion channels

what is Zonisamide (Zonegram) indicated for

Zonisamide (Zonegram) s indicated for tonic-clonic (grand mal) and partial seizures

4 drugs that are primarily used for partial seizures

Gabapentin, Pregabalin, Lacosamide, and Tiagabine

Gabapentin trade name

Gabapentin (Neurontin)

Pregabalin trade name

Pregabalin (lyrica)

Lacosamide trade name

lacosamide (Vimpat)

Tiagabine trade name

Tiagabine (Gabitril)

Gabapentin (Neurontin) and Pregabalin (Lyrica) are similar in structure to what

GABA (inhibitory NT)

Gabaentin (Neurotinin) and Pregabalin (Lyrica) MOA

block CA ion channels and decrease glutamate

Pregabalin (Lyrcia) is indicated for partial seizures and what

Pregabalin (Lyrica) is indicated for partial seizures and nerve pain such as fibromyalgia

Lacosamide (Vimpat) MOA

Lacosamide (Vimpat) enhances the slow inactivation of voltage-sensitive NA channels which decreases electrical signaling

Lacosamide (Vimpat) is indicated for what

Lacosamide (Vimpat) is indicated for partial seizures in 17+ year olds

Tiagabine (Gabitril) MOA

inhibits GABA (inhibitor) reuptake

the three drug classes and the associated drug that treat absence seizures

Succinimides- Ethosuximide (Zarontin)

Oxazolidinediones- Trimethadione (Tridion)

Benzodiazepines- are AC - valium, klonopin, ativan

succinimides drug for absence seizure

Ethosuximide (Zarontin)

what is trade name of Ethosuximide

Ethosuximide (Zarontin)

Ethosuximide (Zarontin) MOA

decreases T-type Ca currents in thalamus

Oxazolidinediones drug that treats absence seizures

Trimethadioine (Tridion)

Trimethadione trade name

Trimethadione (Tridione )

Trimethadione (tridione) MOA

decreases T-type Ca currents in thalamus and is more toxic than succinimides

is trimethadione (tridion) widely used

no trimetadione (tridion) is rarely prescribed because liver and kidney damage are possible side effects

Benziodiazepines are AE/AC/both?

AC

benzodiazepines examples (3)

valium, klonopin, ativan

ativan

benzodiazepine that is go to for status epilepticus

Parkinson's disease

basal ganglia, degeneration of dopaminergic neurons int he substantia nigra

progressive, want to increase dopamine

NT affecting basal ganglia in Parkinson's Disease

DA is low and ACH is high

drugs that form DA (Dopamine) 2

Levodopa (Dopar, Larodopa) and L-Dopa

why can't you just give someone dopamine to treat parkinson's

dopamine cant cross the BBB so you have to find a drug that can and then is metabolized into Dopamine

Levodopa is typically given with what and why

Levodopa (Dopar, Larodopa) is typically given with CARBIDOPA because it hibits dopa decarboxylase

carbidopa does what for levodopa

prevents dopa decarboxylase from breaking it down before it gets to the brain

drugs that inhibit the metabolism of L-dopa and DA - 2 classes

1. Monoamine Oxidase-B Inhibitors

2. Catechol-O-Methyltransferase inhibitors

Monoamine Oxidase-B inhibitors examples (2)

1. Selegiline (Eldepryl)

2. Rasagiline (Azilect)

Selegiline trade name

Selegiline (Eldepryl)

Rasagiline trade name

Rasagiline (Azilect)

Catechol-O-Methyltransferase inhibitors (2)

1. Tolcapone (Tasmar)

2. Stalevo

Tolcapone (tasmar) MOA

inhibits COMT and increases DA

what is Stalevo

a catechol-o-methyltransferase inhibitor that is a combo of L-DOPA, carbidopa, and a COMT inhibitor

DA receptor agonists (3)

1. Bromocriptine (Parlodel)

2. Pramipexole (Mirapex)

3. Apomorphine (Apokyn)

bromocriptine trade name

bromocriptine (parlodel)

bromocriptine (parodel) was the ___ of its kind, which is ___

bromocriptine (parodel) was the 1st of its kind, which are DA agonists

Pramipexole trade name

Pramipexole (Mirapex)

Apomorphine trade name

Apomorphine (Apokyn)

When is Apomorphine (Apokyn) used

Apomorphine (Apokyn) is used during the "off" period when patients have tonic contractions

Amantadine (Symmetrel) is benefical to what disease

Amantadine (Symmetrel) is an antiviral drug that was accidentally found to be beneficial in Parkinson's disease