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106 Cards in this Set

  • Front
  • Back
What does "Autacoids" mean?
Autacoids are mostly LOCAL HORMONES with these 2 main characteristics
1. short duration of action

2. act locally near sites of synthesis or formation
Are Autacoids used clinically as drugs or therapeutic agents?
No, but Autacoid antagonists are used for treating many diseases
-Peptic ulcer
Histamine is found in many plants and animal is it formed?
Decarboxylation of L-histidine

**then either stored or rapidly inactivated
Histamine is mostly bound in granules in what 2 cells?
Mast cells

What are the sites of histamine-containing Mast cells?
Blood vessels
List the 2 important non-mast cell sites of Histamine
1. Brain where histamine acts as a neurotransmitter

2. Enterochromaffin-like cells in the stomach release histamine to stimulate acid secretion from Parietal cells
Bound histamine is inactive but is released by many stimuli to act on surrounding what general mechanisms can histamine be released?
1. Immunologic

2. Chemical

3. Mechanical
Describe the Immunological release of Histamine
1. upon exposure to antigens, plasma cells release IgE
2. IgE binds to IgE receptors on Mast cells
3. Mast cell degranulates to release Histamine, ATP, etc
The Immunologic release of Histamine mediates __1__ and modulates __2__
1. Type 1 allergic rxns

2. acute inflammation
What 2 drugs can displace histamine from Mast cell binding sites without injurying the cell?
1. Morphine

2. Tubocurarine
What are the 3 sites of H1 receptors?
1. Smooth muscle
2. Endothelium
3. Brain
What are the antagonists to the H1 receptor?
1st and 2nd generation H1 blockers
Where are H2 receptors found?
1. Gastric mucosa
2. Mast cells
3. Cardiac muscle
4. Brain
What are the 4 antagonists to the H2 receptors?
What does activation of the H1 receptor cause?
Gq = increase in Intracellular Calcium
What does activation of the H2 receptor cause?
Gs = incrase in intracellular cAMP
Histamine effect on Sensory nerve endings due to H1 receptors
Pain and itching of urticaria
Histamine effect on Arterioles and Precapillary Sphincters due to H1 receptors
Vasodilation ➡ lowers BP ➡ reflex tachycardia
This may cause flushing, warm sensation, or headache
Histamine binding to H1 receptors
Histamine effect on Precapillary vessels due to H1 receptors
dilation of precapillary vessels ➡ increased permeability ➡ edema
Histamine effect on Bronchial smooth muscle due to H1 effects
contraction of bronchial smooth muscle ➡ bronchoconstriction
Histmine effect on GI smooth muscle due to H1 receptors
GI contraction ➡ diarrhea
Histamine effect on the gastric mucosa due to H2 receptors
Gastric Parietal & Intestinal cells ➡ increased GI secretion
Histamine effect on cardiac muscle due to H2 receptors
increased heart rate & contractility
List the 2 mechanisms in which Histamine influences heart rate
Indirectly = via H1 receptors thru REFLEX TACHYCARDIA

Directly = by stimulating cardiac H2 receptors

**direct cardiac stimulation is minimal & H2 antagonists have little or no effect on the heart rate
Describe the Histamine "release inhibitors"
Prophylactics used to protect against allergic rhinitis or bronchoconstriction related to exercise, antigen inhalation, aspirin, or occupational asthma
What are the 2 histamine Release Inhibitors?

Are H1 or H2 antagonists used for allergic reactions such as hay fever, allergic rhinitis, and urticaria?
H1 antagonists
List 2 H1 antagonists that are used for motion sickness but have marked sedative activity


**many of these end in -amine
List 2 H1 antagonists used to prevent MOTION SICKNESS that only have slight sedative effects

List 2 H1 antagonists the have local anesthetic activity

What are they more potent than?
Di-phen-hydramine & Pro-meth-azine

Aside from the H1 antagonistic effects, what other effects do H1 antagonists have? (4)
1. Anti-Parkinsonian
2. Anticholinergic
3. Adrenergic-blocking
4. Serotonin-blocking
What are the most common side-effects of H1 antagonists? (2)
1. Sedation

2. Antimuscarinic activity ➡ urinary retention, blurred vision
What are the less common toxic effects of H1 antagonists? (3)
1. Postural hypotension = Orthostatic hypotension = due to vasodilation

2. Drug allergy

3. Excitation & convulsions in children
List some general properties of 1st generation H1 antagonists
1. older
2. have marked sedative activity
3. often available OTC
4. some are used in pediatrics for sedation
List some general properties of 2nd generation H1 antagonists
1. non-sedating
2. less-lipid soluble = don't cross BBB = less CNS effects
3. less likely to block autonomic receptors
4. little effect on heart, BP, motion sickness, or nausea
List the 4 2nd generation H1 antagonists
1. Cetiri-zine
2. Fexo-fena-dine
3. Lorata-dine
4. Azelastine

What are the 2nd generation H1 antagonists mainly used for?
Hay fever

Allergic rhinitis

2nd generation H1 antagonist used as a nasal spray for seasonal allergic rhinitis and has been shown to be as effective as Fexofenadine
What is the sedation incidence of 2nd generation H1 antagonists vs. 1st generation
7% vs. 50%
What is the main use of the H2 antagonists?
block H2 receptors to reduce gastric acid secretion
-peptic ulcers
-GI hypersecretory disorders
List the 4 H2 antagonists?
1. Cime-tidine
2. Rani-tidine
3. Famo-tidine
4. Niza-tidine

T or F: Doses of H2 antagonists that suppress gastric secretion have a moderate effect on intestinal secretion, heart, or blood vessels
False = they have little or no effect on these
T or F: the side effects of H2 antagonists are infrequent and usually minor
What are the most common side effects of H2 antagonists?
Skin rash
High doses of H2 antagonists may cause these adverse effects
Men = Gynecomastia or Impotence

Women = Galactorrhea = spontaneous release of milk from breasts
Headaches may occur with these 2 H2 antagonists

This H2 antagonist has the fewest side effects
Autacoid that is widely distributed in plant and animal tissues, venoms, and stings
Serotonin = 5-HT = 5-hydroxytryptamine
What is Serotonin formed from?

**then stored or inactivated
Where is 90% of our body 5-HT located?

What other places is it found?
GI Enterochromaffin cells

Blood platelets & raphe nuclei of the brain stem
What is Serotonin the precursor of in the Pineal Gland?
T or F: Many 5-HT receptors have no physiologic function
What are the 2 main functions of 5-HT?
1. GI motility

2. CNS neurotransmitter
What effects does 5-HT have on the Nervous System? (7)
CNS neurotransmitter affecting:
1. sleep
2. sensory perception
3. motor activity
4. temp regulation
5. appetite
6. sexual behavior
7. hormone secretion
What effect does Serotonin have on the 5-HT3 receptors on the Afferent Vagal Nerve endings?
Bezold-Jarisch reflex ➡ bradycardia & hypotension
What effect does Serotonin have on 5-HT3 receptors in the GI and medulla?
Vomiting reflex triggered by cancer chemotherapy drugs
What effect does 5-HT have on Bronchial Smooth muscles?
5-HT effects on the Cardiovascular system:

Generally causes __1__ by stimulating vascular 5-HT2 receptors except in the __2__ & __3__ where vessels are DILATED
1. Vasoconstriction
2. Heart
3. Skeletal muscles
Serotonin effect on:
1. Coronary vessels with endothelial damage
2. Blood pressure
3. Veins
4. Platelets
1. constriction
2. Triphasic = decrease, increase, decrease
3. Constricts veins ➡ increased capillary filling ➡ skin flush
4. causes platelet aggregation via platelet 5-HT2 receptors
Serotonin effect on GI
Contractions from stimulation of 5-HT2 receptors on GI smooth muscles ➡ increased tone & peristaltis
How could 5-HT (Serotonin) cause diarrhea?
Carcinoid tumor overproducing 5-HT = increases GI motility
5-HT(1A) agonist used as an Anxiolytic (anxiety reliever)

"One-pirate in a bus" misses exit 1A which causes him anxiety
Two 5-HT agonists that were widely used as Appetite Suppressants but later withdrawn when serious side-effects of Pulmonary HTN and Valvular lesions occured in young women using them
Fen-fluramine & Dex-fen-fluramine

***when combined with Phenteramine = Fen-Phen
5-HT4 agonist used for GERD and GI motility disorders

**acts through serotonin receptors to increase ACh release at the Myenteric Plexus

**increases esophageal tone, gastric & duodenal contractility
**no longer used due to causing "torsades des pointes"
Selective agonists for 5-HT(1D) and 5-HT(1B) receptors
What are the -Triptan's used for? What is their mechanism?
Acute Migraine Headaches

Constrict Cerebral & Meningeal vessels

**adam TRIPTANS got 1D & 1B on his report card. Mr. TRIPTAN did not get a MIGRAINE due to VASOCONSTRICTION of cerebral vessels
What are the adverse effects of the -Triptan's?
Tingling or warmth sensations
Muscle weakness
Neck pain
Chest discomfort

"adam TRIPTAN had warm tingling feelings in his fingers, was dizzy, couldn't lift weights, and had neck pain & chest discomfort"
What may the -triptan's cause?
Coronary vasospasm and angina
5-HT antagonist that blocks alpha-adrenergic and 5-HT2 receptors
5-HT antagonist that blocks the 5-HT2 and H1 receptors in treatment of Carcinoid tumors, postgastrectomy dumping syndrome, and cold-induced urticaria

**Cyprus 7 treats Carcinoid tumors, postgastrectomy dumping, & cold-induced urticaria
5-HT antagonist that blocks vascular alpha1-adrenergic and platelet 5-HT2 receptors; used for treatment of HTN and vasospastic conditions
5-HT antagonist that blocks 5-HT2 receptors to alter bleeding time and platelet function; used as an antidepressant and for migraine treatment

**"Write on Saran" that causes bleeding, no depression, and no migraine due to Anti-Serotonin 2
3 5-HT antagonists that block 5-HT3 receptors; used for treatment of nausea and vomiting during cancer chemotherapy

**volleyball players SET-RON burgandy up for a spike...he wears 3 "high-tops" (5-HT3) which cause him to fumble around...he has nausea and vomits all over the court due to chemotherapy.
List the 6 Ergot Alkaloid preparations
1. Dihydro-ERGOT-amine
2. ERGO-novine
3. ERGOT-amine mixtures
4. ERGOT-amine tartrate
5. Methyl-ERGO-novine
6. Methy-sERG-ide
What are the Ergot Alkaloids produced by?
Claviceps purpurea
-fungus that infects grain (especially rye), under damp storage
In ancient times, ingestion of contaminated grain resulted in epidemics of Ergotism characterized by these 3 symptoms
1. Hallucination & convulsions
2. Prolonged vasospasm ➡ gangrene and fiery pain
3. Uterine contractions resulting in abortion
What were the Ergot Alkaloids called in the medieval ages? Why?
St. Anthony's fire

named after the saint who provided relief from the burning pain caused by the vasospasm
What are the 2 families of Ergot Alkaloids?
1. Amine alkaloids

2. Peptide alkaloids
What alkaloids are in the Amine category? (3)
1. Ergo-novine
2. Lysergic acid diethy-lamine (LSD)
3. Methy-sERG-ide
Why do patient responses vary widely with Ergot Alkaloids?
1. GI absorption is erratic
2. Variable central and peripheral effects
Ergot Alkaloids can act as partial AGONISTS OR ANTAGONISTS on these receptor types (4)

5-HT(1D) = receptor that causes vasoconstriction

CNS Dopamine receptors

List the 3 peptide ergot alkaloids
1. ERGOT-amine
2. ERGO-cryptine
3. Bromo-criptine
T or F: Ergot Alkaloids may act on presynaptic or postsynaptic sites
What are the CNS effects of Ergot Alkaloids?

What are the sites of action?
Hallucinogens (shown by LSD)

Agonist on pre- or post-jxn 5-HT2 receptors on CNS neurons
What are the Ergot Alkaloid effects on Vascular Smooth Muscle?

What is the mechanism?

stimulation of alpha-adrenergic and 5-HT receptors
Cerebral vessels are very sensitive vasoconstriction by these 4 Ergot Alkaloids

What are they often used for clinically?

Migraine Therapy

**alkaloid MEDS treat migraine
The cerebral vasoconstriction of the Ergot Alkaloids is attributed to the partial agonist effects on these neuronal or vascular receptors (1)
5-HT(1D) receptors
Ergot Alkaloid effects on the Uterus
1. Small doses
2. High doses
1. Rhythmic contraction and relaxation

2. powerful and prolonged contracture due to stimulation of Alpha-adrenergic and 5-HT receptors
Ergot Alkaloids:

As pregnancy progresses __1__ receptors becomes more dominant and uterine sensitivity to Ergot Alkaloids increases

In simulating uterine contractions __2__ is much stronger than other ergot alkaloids
1. Alpha1-adrenergic receptors

2. Ergo-novine
T or F: Bronchial smooth muscles are very sensitive to Ergot Alkaloids, but the GI is unaffected
-Bronchial smooth muscles = unaffected

- GI = very sensitive
What are the most common adverse effects of Ergot Toxicity? What is this due to?
GI disturbances = NVD

Increased GI motility resulting from activation of 5-HT receptors in CNS and GI
What is the most serious toxic effect of Ergot Alkaloids?

What other effects may occur occasionally?
Prolonged vasospasm in arms and legs ➡ gangrene and require amputation

Drowsiness and Hallucinations
What are the 4 general clinical uses of Ergot Alkaloids
1. Migraine treatment
2. Postpartum hemorrhage
3. Hyperprolactinemia
4. GI disorders
The pain onset and relief with Ergot Alkaloids in the treatment of Migraines seem to be related to vasomotor changes that depend on changes in these 2 things
1. Platelet

2. 5-HT
Ergot Alkaloid that is used to treat migraines that produces vasoconstriction and is long-lasting and cumulative

**to minimize cumulative toxicity, doses should not exceed 10 mg/wk
Ergot Alkaloid and Selective Agonists for 5-HT receptors that are used to constrict Cerebral and Meningeal vessels but are not used in patients with Coronary Artery Disease b/c they may constrict coronary blood vessels

-TRIPTAN's = agonists for 5-HT(1D) & 5-HT(1B)
What are some "other" drugs used for migrane prophylaxis?
What are 2 Ca++ channel antagonists that have also been used for migraine treatment?
Flu-nari-zine = for acute treatment

Verap-amil = for prophylaxis
Ergot Alkaloid that produces a powerful & prolonged uterine spasm useful for control of late uterine bleeding
What may happen if Ergonovine is given before the delivery of the fetus?
Maternal and Fetal death incidence may increase
Ergot Alkaloids with high affinity for Pituitary Dopamine D2 receptors used to reduce high Prolactin levels produced by Pituitary tumors (3)
1. Bromo-criptine

2. Caber-goline

3. Per-golide

**Dopamine is released from the Hypothalamus to decrease the release of Prolactin from the Anterior Pituitary
**High Prolactin levels stimulate the release of Dopamine from the Hypothalamus to decrease the release of Prolactin = negative feedback loop
Ergot Alkaloid used as a 5-HT4 receptor agonist used for the treatment of GERD and GI motility disorders

**kid wearing "4 high-tops" has GERD and GI motility disorders, but still has his "SISSY-PRIDE"
Ergot Alkaloid that is a partial 5-HT4 agonist used for treatment of Irritable Bowel Syndrome
3 Serotonin inhibitors that are Selcetive 5-HT3 antagonists used as Antiemetics (anti-nausea/vomiting)