HISTAMINE, 5HT, DOPAMINE MEDS Flashcards by Eva Tran

Where are H1, H2, H3, H4 receptors located?

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“tidine”
Cimetidine
Ranitidine
Nizatidine
Famotidine

H2 Receptor acid reducer (another use for second gen antihistamine)

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Fexofenadine

H2 Receptor Antag/ Second Gen Anti-histamine

ALLEGRA

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Loratadine

H2 Receptor Antag/ Second Gen Anti-histamine

Claritin

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Certirizine

H2 Receptor Antag/ Second Gen Anti-histamine

Zyrtec

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What do you know about H1 Receptor Antagonist/ First Generation Anti-histamines?

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Organ effects of Histamines

CNS?
Heart?
Stomach?
Lungs?
Triple Response (Wheal & Flare)

CNS: H1/ H3—- pain/itch

<3: Vasodilation (Decrease BP) and Reflex tachycardia (increase HR)

Stomach: More stomach fluid produced, Diarrhea induced + GI contractions (move more food/fluid along)

Lungs: Bronchoconstriction

TRIPLE REPONSE / Wheal and Flare
1. REDNESS – microcirculation smooth muscle becomes leaky redness
2. FLUID—Capillary endothelium leady fluid rush in
3. FLARE— Sensory nerve endings flare up

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Recall the major indications for 1st generation antihistamines, and contrast 1st and 2nd generation antihistamine.

Uses of the H2 antihistamines, contrast PPIs

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Serotonin Effects on the Body

CNS?
Resp?
CV?
GI?

Nervous system
-Melatonin precursor
-Vomiting reflex
-Pain and itch (similar to histamine)
– Chemoreceptor reflex
* Bradycardia
* Hypotension

Respiratory
– SEROTONIN Facilitate ACh release – constriction—
– Hyperventilation

CV
– Contraction of vascular SM
* Exception: skeletal muscle, heart (relax)
– Platelet aggregation

GI
– Increases tone MORE TONE = MORE MOVEMENT
– Facilitates peristalsis
– Overproduction – diarrhea

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List the source of serotonin and main 5-HT agonist targets

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Sumatriptan

Describe the action and indication for the use of sumatriptan.

Constrict brain vessels. Migraine caused by brain vessels dilating

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List the three categories of hyperthermia disorders, contributing factors, and treatments.

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Two main 5-HT antagonist targets, and drugs in each category.

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Dopamine Pathways:
1.) Nigrostriatal
2.) Mesolimbic
3.) Mesocortical

Major Dopamine Pathways:
1.) Nigrostriatal—Motor Movement
2.) Mesolimbic– **Reinforcement/Addiction
3.) Mesocortical—Working memory/planning

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Compare and contrast preventatives and treatments for migraine headache

Migraine Prevention
1. Beta-blockers, CCBs, ACEi
2. Antidepressants – SSRIs, TCAs
3. Anti-seizure – Valproate, Topiramate
4. Botox
5. MAbs - Aimovig– blocks CGRP (protein that causes inflammation and vasodilation in brain)

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Ergotamine

Class of medications called ergot alkaloids. It works together with caffeine by preventing blood vessels in the head from expanding and causing headaches.

AKA: For migraine, not as effective as Triptans (5Htr Agonist)

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Chlorpromazine

Anti-nausea – For migraine treatment
You can also use Ondansetron

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5-HT1D/1B Agonist

Uses? Drugs? Major side effects?

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Dex (Fenfluramine)

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Lorcaserin

5 HT2C agonist- WITHDRAWN 2020

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Liraglutide

These are non-serotonin weight loss drugs)
-Liraglutide: GLP-1 Agonist (DM)
-Orlistat: GI Lipase Inhibitor

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Orlistat

These are non-serotonin weight loss drugs
-Liraglutide: GLP-1 Agonist (DM)
-Orlistat: GI Lipase Inhibitor

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Phenoxybenzamine

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Cyproheptadine

Used for?

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Ondansetron (Zofran)

Dopamine How is it made? What is the reuptake transporter? How many receptor types? Main pathway for reinforce behavior?

Major Dopamine Pathways: 1.) Nigrostriatal—Motor Movement 2.) Mesolimbic-- **Reinforcement/Addiction 3.) Mesocortical—Working memory/planning Biosynthesis: Tyrosine** --> LDOPA-> DA DAT, D1-D5

Where in the brain is does the dopamine pathway start?

Where do each of these work?

Fluoxetine (Prozac)*

Citalopram (Celexa) not on study guide

Paroxetine (Paxil) Not on study guide

Sertraline (Zoloft)*

Escitalopram (Lexapro)

Desvenlafaxine (Pristique) **

Duloxetine (Cymbalta)

Phenelzine (Nardil) ***

Selegiline**

Major Seizure Drugs What are their MOA? Uses?

Mechanism of Action of Anti-epileptic Drugs: 1. Modification of ion conductance: Na+, K+, Ca++ 2. Enhancing inhibition: GABA 3. Inhibiting excitation: Glutamate

What drugs would you use first for each?

Partial/ Tonic Clonic *Phenytoin *Fosphenytoin (longer lasting) Focal Seizure: *Carbamazepine *Locosamide (Vimpat) Infant (Focal/Tonic Clonic ONLY) *Phenobarbital *Primidone (derivative) Absent: *Ethosuimide Broad Spectrum: *Valporic Acid *Depakene/Depakote

Phenytoin Fosphenytoin

Carbamazepine

Lacosamide (Vimpat)

Phenobarbital Primidone

GABA ANALOGS Gabapentin Pregabalin Vigabatrin

GABA analog: adjunct for anti-seizures

Other drugs for anti-seizure

Ethosuimide

Valproic Acid Depakene, Depakote

Broad Spectrum Seizure AED

Clonazepam

Drug for epilepsy management

Clorazepate dipotassium (Tranxene)

Benzo

Diazepam Lorazepam

Infantile Spasms? How do you treat? A single seizure episode only?

-More palliative -IM Corticotropins: Prednisone -GABA Analog: Vigabatrin: Leaves GABA around longer, block enzymatic hydrolysis Single Seizure? -Anti-epileptic drugs -Surgery—remove ½ hemisphere (kids adapt better) -Vagus Nerve Stimulation -Ketogenic Diet -------- for kids. Theory: using fatty acid instead of glucose for beta oxidation (slower)

Generalized Tonic- Clonic?? How do we treat? Status Epilepticus? Order of treatment

General Tonic Clonic ~30 mins. Can be LIFE THREATENING! IMMEDIATE MANAGEMENT -IV seizure meds, gaba signaling/ benzodiazepine- treat cardio, resp, metabolic, meds Status Epilepticus: 1.) IV seizure medication: IV diazepam, Lorazepam 2.) LONGER LASTING? IV Fosheynotoin (15-20 mg) (Dilantin derivation) 3.) NOT WORKING?? LARGER DOSE Phenobarbital (20mg/kg)

Anesthesia considerations for seizure meds?

Identify the major subgroups of sedative hypnotics

Classes of Sedative Hypnotic: Name a drug in each Benzodiazepine Barbituates Sleep Aid Anxiolytics Ethanol

GABA Receptor How does it work? How do sedative hypnotics potentiate inhibition?

IPSP Inhibitory synaptic potential

List the four phases of sleep and important changes seen when taking sedative-hypnotics. How does Alc affect the sleep phases?

Alc: More deep sleep phase 4 initially then more REM sleep later Sedative hypnotics: Decrease time to sleep and increase stage 2 non-rem sleep (goal)

Zolpidem

Sedative Hypnotic: AMBIEN *Not a benzo, barb, or narcotic **abuse potential

Eszopiclone

Sedative Hypnotic: LUNESTA *Not a benzo, barb, or narcotic *Abuse potential

Naltrexone

For alcohol dependence

Acamprosate

Adjunct medication for alocholism *Adverse effects: GI symptoms/rash

Disulfiram**

Alcoholism-- makes your hangover worse to make you QUIT!

Buspirone

5-HT1A Receptor Angonist *Relieves anxiety without sedation

Wernicke-Korsakoff Syndrome What symptoms? Other symptoms of neurotoxicity with alc? What's in a banana bag?

Ethanol Pathways: 1. Alcohol Dehydrogenase Pathway 2. Microsomal Ethanol-oxidizing System (MEOS) What drugs would you use? Whats the pathways?

Aripirprazole (Ambilify)

Anti-psychotics

Buspirone

5-HT1A-- serotonin agonist Non-benzodiazepine anxiolytic Slows down serotonin release from raphe nucleus so decrease 5HT. Dont give for depression! only anxiety!!

Benedryl

Histamine 1st gen antagonist Sedation