DR.LEAL - DRUGS WITH IMPORTANT ACTIONS ON SMOOTH MUCLES PART1 Flashcards by Shiela Micah Gascon

released when there are allergies, asthma, and rhinitis, thereby antihistamines are
taken.

HISTAMINE

How well did you know this?

Not at all

Perfectly

Examples of antihistamines:

Cetirizine,
Loratadine
Hydroxyzine

How well did you know this?

Not at all

Perfectly

happy neurotransmitter that affects mood
and sleep

SEROTONIN

How well did you know this?

Not at all

Perfectly

Important mediator of immediate allergic (such as urticaria) and inflammatory reactions (Type I hypersensitivity reactions)

HISTAMINE

How well did you know this?

Not at all

Perfectly

Role in gastric acid secretion
○ Attachment of histamine to H2 receptors
will promote gastric acid secretion; hence,
H2 blockers are given
○ Example of H2 blockers (antacids):
Famotidine, Cimetidine, Ranitidine

HISTAMINE

How well did you know this?

Not at all

Perfectly

anesthetic drug classified under opioids; pain reliever

MORPHINE

How well did you know this?

Not at all

Perfectly

neuromuscular blocking agent

TUBOCURARINE (CURARE)

How well did you know this?

Not at all

Perfectly

requiring energy and calcium
○ A drug that can release histamine in its bulk form

Compound 48/80

How well did you know this?

Not at all

Perfectly

Four Histamine receptors:

○ H1: Smooth muscle, endothelium, brain
○ H2: Gastric mucosa, cardiac muscle, mast
cells, brain
○ H3: Presynaptic autoreceptors and
heteroreceptors: brain, myenteric plexus,
other neurons
○ H4: Eosinophils, neutrophils, CD4 T cells

How well did you know this?

Not at all

Perfectly

Smooth muscle, endothelium, brain

How well did you know this?

Not at all

Perfectly

Gastric mucosa, cardiac muscle, mast
cells, brain

How well did you know this?

Not at all

Perfectly

Presynaptic autoreceptors and
heteroreceptors: brain, myenteric plexus,
other neurons

How well did you know this?

Not at all

Perfectly

Eosinophils, neutrophils, CD4 T cells

How well did you know this?

Not at all

Perfectly

action of histamine on arterioles and
precapillary sphincters
○ Result: ↓ Blood pressure (Anaphylactic shock)
○ Anaphylactic shock: Allergy + Hypotension

VASODILATION

How well did you know this?

Not at all

Perfectly

Intradermal injection of histamine:
characteristic

RED SPOT
EDEMA
FLARE

How well did you know this?

Not at all

Perfectly

vasoconstrictor; have smooth
muscle actions opposite to those of histamine (act on different receptors)

EPINEPHRINE

How well did you know this?

Not at all

Perfectly

causes vasodilation, consequently lowering blood pressure.

HISTAMINE

How well did you know this?

Not at all

Perfectly

a vasoconstrictor, is given to counteract the effects of histamine.

EPINEPHRINE

How well did you know this?

Not at all

Perfectly

○ Drugs that inhibit the release of histamine
○ Reduce the degranulation of mast cells that results from immunologic triggering by antigen-IgE interaction

RELEASE INHIBITORS

How well did you know this?

Not at all

Perfectly

treatment of asthma

CROMOLYN
NEDOCROMIL

How well did you know this?

Not at all

Perfectly

Selective H2-receptor antagonists:
therapy for peptic disease (Ex. antacids -
drugs used for hyperacidity)

Histamine Receptor Antagonists

How well did you know this?

Not at all

Perfectly

Thioperamide and Clobenpropit

H3 RECEPTOR ANTAGONIST

How well did you know this?

Not at all

Perfectly

ANTIHISTAMINE THAT Can cross the blood-brain barrier → effect
in the central nervous system → Strong
sedative effects

1ST GEN

How well did you know this?

Not at all

Perfectly

antihistamine that is Less sedating (reduced distribution into the CNS) treatment of allergic rhinitis and chronic urticaria.
○ Example: Cetirizine

2ndGEN

How well did you know this?

Not at all

Perfectly

H1 antagonists ○ First generation antihistamine

SEDATION

Scopolamine, Dimenhydrinate ○ Prevents motion sickness ○ Example: Bonamine® generic name: meclizine hydrochloride

Antinausea and antiemetic actions

- Significant acute suppressant effects on the extrapyramidal symptoms associated with certain antipsychotic drugs - Can also be used to sedate the patient

Diphenhydramine

Significant atropine-like effects on peripheral muscarinic receptors - During an allergic reaction, the patient can experience drooling. Atropine-like action of antihistamine can cause dry mouth, increased heart rate, etc.

Antimuscarinic actions ○Ethanolamine and Ethylenediamine

- Alpha-receptor-blocking (orthostatic hypotension) - Used during painful labor of pregnant women. It has localized anesthetic activity and sedative. This can be used to lessen the pain of labor.

Promethazine

Inhibit mast cell release of histamine and some other mediators of inflammation

CETIRIZINE

found in the gastric mucosa. Once histamine is released and attached to the H2 receptors, they promote gastric acid secretion.

H2 RECEPTORS

Medicine used to counteract histamine-2 receptors are:

○ Cimetidine (Prototype) ○ Ranitidine ○ Famotidine ○ Nizatidine

● Blocks H2 receptors ● Relatively selective or specific to H2 receptor only, have no significant blocking actions at H1 or autonomic receptors

Histamine H2 Antagonist

is the drug usually given to treat hyperacidity. H2 blockers can be an alternative drug for hyperacidity

OMEPRAZOLE

Has significant antiandrogen effects in patients receiving high doses. - Can cause gynecomastia on male patients.

CIMETIDINE

○ Has a weaker inhibitory effect on hepatic drug metabolism ○ No androgenic effects ○ Safer

RANITIDINE

● Important neurotransmitter in the CNS and and Enteric NS (GI Tract nervous system) ● A local hormone in the gut ● A component of the platelet clotting process ● Play a role in migraine headache

SEROTONIN (5-HYDROXYTRYPTAMINE; 5-HT) & RELATED AGONISTS

neoplasm (cancer) of enterochromaffin cells in the gastrointestinal tract that produce large amounts of serotonin. ○ High levels of serotonin play a role in migraine headache.

CARCINOID SYNDROME

rate-limiting step ON SYNTHESIS OF SEROTONIN

Hydroxylation by tryptophan hydroxylase-1:

neoplasm in the GIT

CARCINOID SYNDROME

CARCINOID SYNDROME TRIAD

DIARRHEA FLUSHING CARDIAC INVOLVEMENT

To treat diarrhea of patients with carcinoid syndrome would be

telotristat ethyl.

○ Orally active hydroxylase inhibitor ○ Approved for the treatment of diarrhea due to carcinoid tumor

Telotristat ethyl

sleeping pill that has selectivity for Melatonin 1 receptor and Melatonin 2 receptors.

RAMELTEON

Spinal anesthesia blocks T4 down to extremities. Upon blocking the T4 level, the cardioaccelerators are also blocked, hence lowering heart rate then blood pressure.

Bezold-Jarisch Reflex

powerful vasoconstrictor except in skeletal muscle and the heart (dilates blood vessels) resulting to a decrease in blood pressure

SEROTONIN

Powerful stimulant of gastrointestinal smooth muscle, increasing tone and facilitating peristalsis causing diarrhea

SEROTONIN

● Excess serotonergic activity in the central nervous system ● Skeletal muscle contractions / muscle rigidity caused by serotonergic activity in the CNS.

SEROTONIN SYNDROME

Malignant hyperthermia DOC

DANTROLENE

○ Most important in the brain and mediate synaptic inhibition via increased potassium conductance ○ Always remember that serotonin 1 receptors are located in the brain or the CNS

5HT1 receptors

○ Important in both brain and peripheral tissues

5HT2 receptors

Found in the CNS, especially in the chemoreceptive area and vomiting center,

5HT3 receptors

setron” from serotonin; an antiemetic drug used in cancer patients. - They block serotonin in the serotonin 3 receptor

Ondansetron

○ A 5 HT1A agonist ○ Drug that helps the attachment of serotonin to the 5HT1A receptor ○ Effective nonbenzodiazepine anxiolytic

BUSPIRONE

○ selective 5 HT agonist ○ appetite suppressant but was withdrawn because of cardiac valvulopathy

Dexfenfluramine

○ a 5 HT2C agonist ○ weight loss medication

Lorcaserin

○ α adrenoceptors and serotonin receptor blocking effects ○ Used in pheochromocytoma

Phenoxybenzamine

treatment of the smooth muscle manifestations of carcinoid tumor and in cold induced urticaria

Cyproheptadine

○ ○ prototypical 5 HT3 antagonist prevention of nausea and vomiting associated with surgery and cancer chemotherapy

Ondansetron

aura of variable duration, followed by severe throbbing unilateral headache that lasts for a few hours to 1-2 days

MigraineHeadache

in migraine headache trigeminal nerve distribution to intracranial (and possibly extracranial) arteries releases

calcitonin gene related peptide (CGRP; powerful vasodilator)

MIGRAINE TREATMENTS

○ 5 HT1D/1B agonists (sumatriptan) ○ Ergot alkaloids ○ NSAIDs (Ex. Mefenamic acid, celecoxib) ○ β adrenoceptor blockers ○ Calcium channel blockers ○ TCA ○ SSRIs ○ Antiseizure agents

● produced by Claviceps purpurea, a fungus that infects grasses and grains especially rye under damp growing or storage conditions ● synthesizes histamine, acetylcholine, tyramine

ERGOT ALKALOIDS

○ dementia with florid hallucinations; prolonged vasospasm, which may result in gangrene; and stimulation of uterine smooth muscle, which in pregnancy may result in abortion

Ergotism (St. Anthony’s Fire/Holy Fire)

ORGAN SYSTEMS EFFECTS ○ Synthetic ergot compound ○ Hallucinogen

Lysergic Acid Diethylamide (LSD; “acid”)

ORGAN SYSTEM EFFECTS OF ERGOTS ○ Suppress prolactin secretion from pituitary cells by activating regulatory dopamine receptors ○ Bromocriptine 2.5 mg BID or TID ○ Peripartum cardiomyopathy

Bromocriptine, Cabergoline, and Pergolide

○ Constrict vessels (prolonged vasospasm) ○ Prevent vascular headache ○ blocked by α blocking agents ERGOT EFFECTS

ERGOTAMINE

ERGOT EFFECTS ○ For uterine contraction ○ Postpartum Hemorrhage (2nd choice) ○ Oxytocin (1st choice)

ERGONOVINE

3RD CHOICE FOR POSTPARTUM HEMORRHAGE

CARBOPROST

produce prompt vasoconstriction during coronary angiography

ERGOT ALKALOIDS

ERGOT ALKALOID FOR used in the treatment of Alzheimer’s dementia

ERGONOVINE

1. Serotonin antagonists include the following, except a. Phenoxybenzamine b. Cyproheptadine c. Ergonovine d. Ondansetron

C. ERGONOVINE

Which of the following is not a serotonin agonist a. Buspirone b. Dexfenfluramine c. Ergotamine d. Lorcaserin

C. ERGOTAMINE

Which receptor is the most important in the brain and mediates synaptic inhibition via increased potassium conductance a. 5HT2 b. 5HT4 c. 5HT1 d. 5HT11

C. 5HT1

The following are effects of Bromocriptine, Cabergoline, and Pergolide, except: a. Suppress prolactin secretion from pituitary cells by activating regulatory dopamine receptors b. Bromocriptine 2.5 mg BID or TID c. Peripartum cardiomyopathy d. AOTA e. NOTA

E. NOTA ALLARE FOR Bromocriptine, Cabergoline, and Pergolide

Whichcorresponding location in the body? histamine receptor is correctly paired with its a. H1: cardiac muscle b. H2: smooth muscle c. H3: brain d. H4: gastric mucosa

C. H3:BRAIN

Drug that prevents nausea and vomiting associated with surgery and cancer chemotherapy a. Buspirone b. Ondansetron c. Bromocriptine d. Ergonovine

B. ODANSETRON

Used to treat diarrhea in patients with carcinoid syndrome Loratadine Odansetron Dexfenfluramine Telotristat ethyl

Telotristat ethyl

A potent vasodilator released in migraine headaches Histamine Calcitonin gene related peptide (CGRP) Methysergide p-chlorophenylalanine (PCP)

Calcitonin gene related peptide (CGRP)

Considered the 2nd choice for the management of postpartum hemorrhage a. Ergonovine b. Cabergoline c. Pergolide d. LSD

A. ERGONOVINE

Serotonin antagonist used in pheochromocytoma a. Cyproheptadine b. Odansetron c. Phenoxybenzamine d. Dexfenfluramine

c. Phenoxybenzamine

DR.LEAL - DRUGS WITH IMPORTANT ACTIONS ON SMOOTH MUCLES PART1 Flashcards

(81 cards)