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Pharmacology
Autoacoids
80
Pharmacology
Graduate
07/26/2014

Additional Pharmacology Flashcards

 


 

Cards

Term
3 primary autocoids
Definition

prostaglandins

histamine

serotonin

Term
Important neurotransmitter in the brain but it in the body it is a chemical that is released and causes closed action activity
Definition
serotonin
Term
A form of signaling in which a cell secretes a chemical messenger that signals the same cell
Definition
autocrine
Term
local mediators
Definition

autocrine

paracrine

Term
a form of signaling in which the targt cell is close to the signal releasing cell
Definition
paracrine
Term
Rapidly destroyed or removed
Definition
histamine and prostaglandins
Term
hormones secreted into the bloodstream
Definition
endocrine
Term
All of paracrine and autocrine are considered....
Definition
autocoids
Term
Which is more broad..autocrine or paracrine?
Definition
paracrine
Term
Synthesized locally and have drugs that block them called antihistamines
Definition
autocoids
Term
Therapeutic uses of prostaglandins
Definition

abortion

peptic ulcers

erectile dysfunction

glaucoma

Term
which prostaglandin is used for abortion
Definition
misoprostol (Cytotec)
Term
Which prostaglandin is used for peptic ulcers?
Definition
misoprostol (cytotec)
Term
How does misoprostol help peptic ulcer?
Definition

inhibits secretion of HCl associated with NSAIDS problem with adverse effects

 

Term
Which prostaglandin is used for erectile dysfunction
Definition

alprostadil

injection

Term
Where are histamines located?
Definition

in nearly all tissues

high in-lungs, skin, GI tract 

Mast cells

basophils

In venoms from insect stings

Term
Rapidly destroyed by amine oxidase enzymes
Definition
histamine
Term
One of several chemical mediators released from tissues by destruction of cells as a result of cold, bacterial toxins, bee sting venoms, trauma, anaphylaxis, and allergies
Definition
histamine
Term
Mechanism of action of histamine
Definition

G protein mediated systems

binds two types of receptors, H1 and H2

Term
H1 receptors
Definition

capillary permeability- nasal secretions

smooth muscle contraction- bronchiole constriction

intestinal cramps, diarrhea

itch and pain

Term
H2 receptors
Definition

decrease TPR

increase HR

increase inotropy

acid secretion

Term
triple response
Definition

dilate capillaries (H1)

flare, reddening (H1/H2)

edema (wheal) (H1)

Term
Histamine's role in anaphylaxis and allergy
Definition

contraction of smooth muscle

stimulation of secretions

dilation and increased permeability of capillaries

stimulation of sensory nerve endings

Term
Mediators of anaphylaxis and allergies
Definition

histamine

serotonins

leukotrienes

ECFA (eosinophil chemotaxic factor of anaphylaxis)

Term
Release of mediators from storage sites may cause...
Definition
local reaction or system reaction
Term
Slow release of mediators allows...
Definition
rapid inactivation and local reaction
Term
Fast release of mediators leads to the entry of mediators into the bloodstream with...
Definition
subsequent anaphylaxis
Term
Classic antihistmaines
Definition
H1 receptor blockers
Term
Which generation (1st and 2nd) has better efficacy?
Definition
neither they have equivalent efficacies
Term
Which generation has additional effects unrelated to blocking H1 receptors
Definition
1st generation
Term
What are the additional effects of the 1st generation H1 receptor blockers?
Definition

antimuscarinic

alpha blockers

serotonin receptor blockers

No H2 blockade

diphenhydramine good local anesthetic

Term
second generation H1 antihistamines
Definition

fexofenadine (Allegra)

Loratidine (Claritin)

Desloratidine (Clarinex)

Cetrizine (Zyrtec)

Term
1st generation H1 antihistamines
Definition

diphenhydramine (Benadryl)

Dimenhydrinate (Dramamine)

Chlorpheniramine (Chlortrimeton)

Meclizine (Antivert)

Cyproheptadine (Perivert)

Promethazine (Phenergan)

Hydroxyzine (Atarax)

Term
Which H1 antihistamines were removed from U.S. market?
Definition

terfenadine (Seldane)

Astemizol (hismanal)

Both 1st generation

Term
Why were the two H1 antihistamines removed from the market?
Definition

because they were prolonging the QT interval 

polymorphic ventricular tachycardia

torsades de pue

 

Term
Useful in treating allergies caused by antigens acting on IgE-antibody sensitized mast cells
Definition
antihistamine
Term
useful in treating allergic rhinitis and urticaria
Definition
antihistamine
Term
Not used in asthma bcause it only has one of several mediators of asthma
Definition
antihistamine
Term
not used in anaphylaxis because epinephrine is used instead
Definition
antihistamine
Term
1st generation drugs used in motion sickness and nausea
Definition

diphenhydramine (benadryl)

dimenhydrinate

cyclizine

meclizine

hydroxyzine

Term
Prevent or diminish vomiting and nausea mediated by chemoreceptor and vestibular pathways
Definition
1st generation antihistamines for motion sickness and nausea
Term
Which H1 blocker is a somnifacient?
Definition
diphenhydramine
Term
Which H1 drug has strong sedative properties and may be used in the treatment of insomnia
Definition
diphenhydramine (benadryl)
Term

Absorbed orally

average 1/2 life of 4-6 hours

distributed in all tissues including CNS

metabolized in liver (CYP 450)

excreted in urine

Definition

cetrizine (Zyrtec)

fexofendaine (allegra)

Term
Sedation adverse effects of antihistamines
Definition
tinnitus, fatigue, dizziness, lassitude, incoordination, blurred vision, tremors
Term
Sedation is less with 1st generation or 2nd generation? why?
Definition

2nd generation

penetrates poorly in the CNS

Term
more adverse effects of antihistamines (H1)
Definition

dry mouth

weak anticholinergic effects may lead to dry mouth and nasal mucosa

Term

May potentiate other CNS depressants 

should not be used wit MAO inhibitors

Definition
antihistamines (H1)
Term
Why should antihistamines (H1) not be used with MAO inhibitors
Definition
it doubles the effects because it blocks muscarinic receptors twice potentially
Term
Overdoses of anthistamines (H1) effects
Definition

high margin of safety

main concern w/ children 

CNS- hallucinations, excitement, ataxia, convulsions

 

Term
untreated overdose of antihistamines (H1) may lead to..
Definition
deepening coma and cardiorespiratory collapse
Term
Do H2 receptor blockers have affinity for H1?
Definition
little or no affinity
Term
Do H2 receptor blockers inhibit/stimulate acid secretion
Definition
stimulate
Term
H2 receptor blockers examples
Definition

cimetidine

rantidine

famotidine

nizatidine

Term
Which drug interfers with hepatic metabolism and has anti androgenic effects (competes with mal sex steroids)
Definition
cimetidine
Term
Distinguising features of migraine
Definition

usually unilateral

pulsatile

throbbing pain

Term
Types of migraines
Definition

migraine with aura

migraine without aura

Term
Which migraine is referred to as a common migraine?
Definition
migraine without aura
Term
which type of migraine is referred to as a classic migraine?
Definition
migraine with aura
Term
what percentage of migraines are without aura?
Definition
85%
Term
MOA- Vasoconstriction of meninges or inhibition of neuropeptide release (Substance P)
Definition
sumatriptan (imitrex)
Term
Sumatriptan is effective in what percentage of patients?
Definition
70%
Term
Sumatriptan is an agonist for which receptor?
Definition
Serotonin 5-HT1D
Term
Which drug acts on found on peripheral nerves that innervate the intracranial vasculature
Definition
sumatriptan
Term
How can sumatriptan be administered
Definition
subcutaneous, intra-nasal, orally
Term
This drug has a short half life and a headache may recur in 24-48 hours
Definition
sumatriptan
Term
Which drugs are the serotonin receptor agonists
Definition

triptans

Naratriptan

Rizatriptan

Eletriptan

Forvatrpin

Almotriptan

Zolmitriptan

Term
Hives, difficulty breathing, swelling of your face, lips, tongue, or throat- angioedema
Definition

allergic reactions (sulfonamide)

sumatriptan

Term
Confusion, hallucinations, fast heart beat, feeling faint, fever, sweating, muscle spasm, difficulty walking, and/or diarrhea
Definition
serotonin syndrome
Term
Which drugs have serious side effects on the heart, including heart attack or stroke
Definition
sumatriptan
Term
stomach pain and bloody diarrhea
Definition
sumatriptan
Term

Derivative of ergotamine

IV

nausea is a common side effect

Definition
dihydroergotamine
Term
Similar actions as sumatriptan but less 5- HT receptor selectivity
Definition
dihydroergotamine
Term

Sides effects are diarrhea, nausea, or vomiting 

avoid in pregnancy and CAD

Definition
dihydroergotamine
Term
Relieve attack of acute migraine
Definition

NSAIDS - prostaglandin inhibitors

aspirin, naproxen, ibruprofen

Term
Prochlorperazine (Compro) used for migraines
Definition

antimetic

dopamine 2 antagonist

Term
Rescue agents used for migraines
Definition

opiods

codeine, meriperidine

last option if NOTHING else works

Term

Indicated if attacks occur two or greater tmes per month or if severe or complicated by neurologic signs

 

Definition
prophylactic treatment of migraine
Term
Which two drugs were mentioned when talking about prophylactic treatment of migraine
Definition

Beta blockers (esp propranolol)

depakote ER (valproate/valproic acid)

Term

Extended release product

no evidence that it is useful in the acute tx of migraines

should not be used in women who are pregnant

Definition
depakote ER
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