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FIU Opiates and Serotonin
Opiate and Serotonin receptor drugs
52
Pharmacology
Professional
12/12/2011

Additional Pharmacology Flashcards

 


 

Cards

Term
Stimulate pain receptors
Definition

Capsaisin (chilli peppers)

H+ < 7.0

Temperature increase

Term
Classes of endogenous opioid peptides that modulate nociception via opiod receptors
Definition

Enkephaline

Endorphine

Dynorphine

 

 

Mnemonic: Pain in the END because he DYN-ed (dined) on ENK (ink) EF (of) the pen.

Term
Endorphines have the highest affinity for these receptors
Definition
μ opiod receptors that open supraspinal K+ channels, leading to hyperpolarization
Term
Opioid μ receptor effects
Definition

-Supraspinal and spinal analgesia

-Parasympathetic nervous system activation including ...

--euphoria, respiratory depression, bradycardia, obstipation (failure to pass stool/gas), urinary retention, mitosis (constricting of pupils), also addiction due to europhoria

Term
Enkephalines have the highest affinity for these receptors.
Definition
δ opioid receptors which moduated the activity of μ receptors.
Term
Dynorphines have the highest affinity for these receptors.
Definition
spinal κ receptors which inhibit Ca2+ channels and decrease neurotransmitter release
Term
opioid κ receptor effects
Definition

-analgesia

-dysphoria (therfore not addictive)

-psychotomimetic effects (delusions, delirium, etc)

Term
Metabolism of endogenous opioid peptites is done by these.
Definition
Membrane neuropeptidases that cleave at the amino terminal tyrosine residue, resulting in an ultra-fast half life that prevents endogenous addiction.
Term

Morphine

-Mode of action

-Effects

-Side Effects

-Metabolism, half-life, analgesic potency

Definition

-μ opioid receptors

-μ mediated effects (analgesia, PNS stimulation, addiction)

-itching (histamine release due to mast cell stimulation, emesis (D receptor agonist)

-Phase 2 in liver, t1/2 = short 3 hr, 1.0 Mo

Term

Piritramid (Dipidolor)

-Mode of action

-Effects

-Side Effects

-analgesic potency

Definition

-μ opioid receptors

-μ mediated effects (analgesia, PNS stimulation, addiction)

-LESS THAN morphine: itching (BUT LESS histamine release than morphine), emesis (D receptor agonist)

-0.8 Mo

 

 

 

 

Term

Codeine (Methyl-morphine)

-Mode of action

-Effects

-Side Effects

-metabolism, analgesic potency

Definition

-10% converted to morphine which acts on μ opioid receptors

-μ mediated effects (analgesia, PNS stimulation, addiction)

-itching (histamine release), emesis (D receptor agonist)

-hepatic (3A4 & 2D6), 0.1 Mo

Term

Tramadal

-Mode of action

-Effects

 

 

Definition

-MIXED: 1) metabolism by 2D6 to agonist that acts on μ opioid receptors; 2) Inhibition of norephinephrine (NA: noradrenaline) and Serotonin (5-HT) reuptake i.e. they are NASRI's (Noradrenaline-Serotonin Reuptake inhibitors) 3) central α2 agonist (Clonidine-like) which slows release of SNS neurotransmitters

-1) μ mediated effects (analgesic: especially for acute pain) 2) relieves chronic pain 3) slows SNS

 

 

Term

Pentazocine (Fortral)

-Mode of action

-Effects

-Side effects

Definition

-MIXED opioid: κ receptor agonist; μ receptors weak antagonist

-analgesia

-dysphoria, can cause withdrawal syndrone in mophine abusers

 

Term

Methadone

-Mode of action

-Effect

-Side effects

-half-life; analgesic potency

Definition

-MIXED: opioid μ receptors agonist; NMDA antagonist

-analgesia, used to reduce opioid abuse/sedation (because long acting)

-unpredictable effects

-slow acting, variable half life (6-8 hr), but active metabolite t1/2 = 55 hr leading to accumulationand sedation; 4-12 Mo

Term

Remifentanil

-Mode of action

-Half life and potency

-Delivery method

Definition

-Opioid μ receptor agonist

-Ultra-short (stays in blood and requires continuous infusion because metabolized by esterases); 100 Mo

-Intravenous (IV)

Term

Pethidin/Meperidine

-Mode of action

-Effect

-Side effects

-Half life and potency

-Delivery method note

Definition

-MIXED: 1) anti-cholinergenic; 2) SSRI; 3) alpha-blocker; 4) interaction with MAO-I

-1) atropine-like effects e.g. causes mydriasis (pupil dilation)...Only opioid that does this (usually stimulates PSN...ALSO prevents post-anesthetic shivering; 3) vasodilation; 4)increase catelcholamines

-Normeperidine is neurotoxic and can accumulate with renal insufficiency

-short t1/2= 2hr, 1/20 Mo

 

Term

Noloxone

-Mode of action

-Effect

Definition

-Opioid competitive antagonist

-Stops respiratory depression

Term

Causes of emesis

--Treatment

Definition

-GI tract afferent stimulation of 5-HT3 (Serotonin) receptor in CRTZ

-Stimulation of dopamine receptors in CRTZ (chemoreceptor trigger zone in medulla)

-Vestibular nucleus release of Ach which stimulates Muscarinic receptors in CRTZ

--Commonly treat with 5-HT3 and D2 (dopamine receptor) blockers...muscarinic blocker only for motion sickness

Term

setron (ending)

-Mode of action

-Effect

Definition

-5HT3 antagonist

-anti-emesis

Term

Droperidol (DHB)

Metoclopramid (Pasertin)

-Mode of action

-Effect

Definition

-D2 antagonist (also 5-HT3 antagonist and 5HT4 agonist)

-Anti-emetic

 

Term

Scopolomine

-mode of action

-effect

Definition

-muscarinic antagonist (affecting vestibular nucleus and CRTZ)

-for motion sickness only

Term

Diphenhydramine (Benadryl)

-Mode of action

-Effect

-Side effect

Definition

-H1 blocker (antimuscarinic agent like those in vestibular nucleus)

-anti-emesis (motion sickness only)

-makes sleepy (but hard to wake up)

Term
Atropine can be used for anti-emesis but isn't for these reasons
Definition

-ROSA (rapid onset, short acting)

-normally raises HR, but in low doses, inhibits pre-synaptic Ach receptors (which when activated, stop the release of Ach). This leads to an increase in Ach (which stimulates PNS) and causes bradycardia

Term
Increased atropine causes these effects
Definition

-Central anti-cholinergenic syndrome

--dry as a bone (can't sweat because Ach in SNS stimulates sweat glands)

--red as a beet (vasodilation to release heat, because Ach in PNS causes vasoconstriction)

--hot as a hare (body heat increases, Ach in PNS thru thalamus causes response to heat)

--blind as a bat

--mad as a hatter (CNS effect)

Term

5 HT receptors

-endogenous agonist

-tropic types

Definition

-Serotonin receptors influencing metabolic processes

-5-HT3 are ionotropic, all others are metabotropic

Term

5-HT

-Receptor type, mode of action for each, effect for each (Example for each)

Definition

1) 5-HT 1A, agonist->Gi -> inhibit AC (adrenylyl cyclase, anxiety (pirones) and hypertension (pidil)

2) 1D/1F, agonist, migrane (triptans)

3) 2, antagonist, psychosis

4) 3, antagonist: blocking afferent pathways from GI tract, emesis (setrons)

5) 4, agonist, gastroparesis (prides, esp. to help diabetics with vagus nerve damage)

6) RI, ..., depression

 

Term

Urapidil

-Mode of action

-Effect

Definition

-DUAL: 5-HT 1A agonist (α1 adrenoreceptor antagonist)

-vasodilation, BP down

Term

Buspirone

-Mode of action

-Effect

-Onset

Definition

-5-HT IA partial agonist (also D2 and weak 5-HT2 affinity)

-anti-anxiety (for chronic anxiety; as opposed to benzodiazepines for acute anxiety)

-slow onset (4-6 weeks), effect may be delayed for several months

Term

Triptans (e.g. Sumatriptan)

-Mode of action

-Effect

-Metabolism

-Example with long half life

-Delivery method with best theraputic gain

-Contraindication

Definition

-5-HT1 B or D

-agonists

-1B: arterial (cerebral) vasoconstriction; 1D: reduce nociceptive transmission (inflammatory soup)

-anti-migrane (vasodilation and inflammation cause pain...for acute migrane only)

-usually Monoamine oxidase aka MAO-A (except Naratriptan: CYP only), causes interaction with NE which is MAO-A metabolized too...dopamine is MAO-B metabolized

-Frovatriptan: t1/2 = 25 hr

-subcutaneous

-cardiovascular disease: vasoconstriction bad for those with coronary artery disease, impared infusion etc

Term

Moclobemide (Aurorix)

-Mode of action, effect

Selegeline (Antiparkin)

-Mode of action, effect, side effect

 

Definition

-MAO-A inhibitor which increases serotonin, anti-depressant

-MAO-B inhibitor which increases dopamine, anti-Parkinson Disease but in high amounts psychotic effect

Term

St. John's wort (Hyperforin)

-MAO interaction
-CYP interaction

Definition

-MAO-A inhibitor = antidepressant

-CYP450 3A4 inducer

Term

5-HT2

-tropic type

Definition
-metabotropic: Gi protein-coupled receptor that activates protein lipase C, which releases DAG (diacylglycerol) and IP3 (inositol triphosphate), stimulating PKC (protein kinase C) and Ca2+ release
Term

Pizotifen( Sanomigran, Pizofen)

-Mode of action

-Effect

Definition

-5-HT2 antagonist (and 5-HT1 antagonist)

-prophylaxis of migraines (prevents vasodilation)

Term

Mianserin and Ritanserin

-Mode of action

-Effect

Definition

-5-HT2 antagonist

-CNS drug for anxiety and depression (tricyclic-esque)

Term

Ketanserin

-mode of action

-effect

-side effect

Definition

-5-HT3 antagonist (and α1 blocker)

-Anti-hypertensive (vasodilator)

-Raynaud disease: mostly females get, spasms of finger arteries controlled by α1 receptors.

Term

Nefazadone (Serzone)

-mode of action

-effect

-side effect

Definition

-MIXED: 5-HT2 antagonist and SSRI (Selective seretonin reuptake inhibitor)

-antidepressant

-liver damage (removed from market)

Term

Trazodone (-zodone)

-mode of action

-effect

-side effect?

Definition

-MIXED: 5-HT2 antagonist and SSRI (Selective seretonin reuptake inhibitor)

-antidepressant

-without liver toxicity of Nefazodone

Term

Quetiapine, Olanzapine, Ziprasidone

-mode of action

-effect

-side effects

Definition

-1) D2 ≈ 5-HT2 2) D2 < 5-HT2 3) D2 << 5-HT2

-antipsychotic

-the less it relies on D2 blockage, the less D2 blocker effects e.g. Parkinson-like effects.

Term

Aripiprazole

-Mode of action

-effect

-side effects?

Definition

-5HT1A agonist, 5-HT2 antagonist (inbitory and blocked excitatory

-dopamine-serotonin system stabilizer

-no associated with significant weight gain or prolonged QT

Term

Setrons

-mode of action

-effects

-Important examples

 

Definition

-5-HT3 blocker (closes Na+, Ca 2+ and K+ channels)

-anti-emesis

-Palonosetron (long acting, single IV dose before chemotherapy), Alosetron (causes IBS/diarrhea)

Term

5-HT4 receptor activation causes the release of this.

-ending?

 

Definition

Acetylcholine (through Gs protein-coupled receptor and production of cAMP)

-pride

Term

Metoclopramide

-mode of action

-effects

-side effects

Definition

-5-HT4 agonist, D2 antagonist, weak 5-HT3 antagonist, ChE inhibitor

-increase Acetylcholine, promoting gastric emptying

-tardive dyskinesia (abnormal movements which are Parkinson-like that have a late onset; occur with antipsychotic drugs also as a result of D2 blockade.)

Term

Cisapride

-Mode of action

-Effect

-Side effects

Definition

-5-HT4 antagonist

-increases Ach release

-doesn't effect D2 receptors and so no tardive dyskinesia, however caused arrhythmias and death due to interference with the metabolism of K+ channel blockers which cause hyperpolarization and prolonged QT

Term

Mosapride

-Mode of action

-Effect

-Side effects?

Definition

-5-HT4 antagonist

-increases Ach release which promotes gastric emptying (esp. prescribed to diabetics with neuropathy)

-doesn't interfere with the metabolism of K+ channel blockers

Term
Itopride
Definition

-Acetylcholine esterase inhibitor, D2 antagonist

-prevents Ach metabolism (effects PNS and sweating)

 

Term

Tegaserod

-mode of action

-effect

-side effect

Definition

-5-HT4 agonist; 5-HT2A antagonist

-increase Ach, vasoconstriction

-angina, heart attack, stroke, serious cases of diarrhea, ischemic colitis

Term
Serotonin transporter mechanism
Definition
SERT enables 5-HT (Serotonin) reuptake. Serotonin binds along with Na+ and Cl-. Transporter flips inside and releases serotonin. K+ binds to the transporter and it flips back out.
Term

Selective Serotonin Reuptake inhibitors

-mode of action

-effect

-side effects

-examples

Definition

-increases 5-HT (can inhibit reuptake of NE if not selective)

-anti-depressant

-Rare and almost never lethal (as opposed to TCAs), hyperthermia, autonomic dysfunction

-Fluoxetine (Prozac), Sertralin (Zoloft), Citalopram (Cipramil): most selective

Term

Dapoxetine (Priligy)

-mode of action

-effect

-side effect?

Definition

-SSRI

-anti-depressant

-delayed ejaculation

Term

SSRI

-metabolism

-interaction

Definition

-metabolized by mainly CYP 450 2D6 except Citalopram (3A4)

-Sertraline (Zoloft) and Citalopram do not interact with any CYP 450 enzyme

Term

Venlafaxin (Effexor)

-mode of action

-effect

Definition

-NASRI that increases NE(NA) and 5-HT

-anti-depressant ("clean TCA": effect of TCA without side effects or structure), for chronic pain

Term

Duloxetine (Cymbalta)

-Mode of action

-Effect

Definition

-NASRI that increases NE(NA) and 5-HT

-anti-depressant ("clean TCA": effect of TCA without side effects or structure), for chronic pain

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