Term
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Definition
They work on the neighboring cells and primarily travel through a local tissue. |
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Term
Explain histamine storage and release. |
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Definition
It is found in mast cells (skin, intestinal mucosa, and lung mucosa) and basophils in blood.
Histamine is immediately released upon synthesis. |
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Term
What are three histamine subtype that mediate the response? |
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Definition
H1(IP3, phospholipase C, DAG, Ca)
H2 (increased adenylate cyclase)
H3 (decrease adenylate cyclase ) |
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Term
Explain Physiological responses of histamine |
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Definition
Allergic response stimulates release of Substance P from the C fibers causes itching and increases capillary permeability.
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Term
Explain the vasodilation during allergic response by H1 receptors. |
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Definition
H1: NO, PGI2 release and gives rapid onset mediated by calcium
H2. relaxes vascular smooth by cAMP and longer lasting. |
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Term
What responses are mediated by H1 receptor? |
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Definition
Triple response; Flush, flare and wheal.
causes constriction of extravascular smooth muscle. Bronchoconstriction and diarrhea |
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Term
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Definition
promoting the secretion of gastric acid in the intestines. |
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Term
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Definition
Presynaptic response is mediated by H3 receptors. Involved in arousal and wakefulness. |
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Term
Explain the therapeutic affects of H1 antagonists
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Definition
Allergic response and have no affect on acute allergic response such as anaphylaxis
sedative and used in sleeping.
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Term
What are some therapeutic uses of non H1 mechanism |
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Definition
Non-allergic rhinorhea (work by blocking muscarinic receptors)
Motion sickness prevention by blocking cholinergic activity
Parkinson's by blocking dopaminergic receptors
Antienematic by blocking dopaminergic receptors
and block Na channels for anesthesia |
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Term
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Definition
Sedation.
Dry mouth, urinary retention, and blurred vision due to blocking of muscarinic receptor
CNS excitation mostly for elderly patients.
Tolerance
Gastrointestinal |
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Term
What is Torsades De pointes |
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Definition
It is cardiac toxicity and it is caused by the lenghtening of QT and massive de-polarization followed by small repolarization.
It is caused by using astemizole or terfanadine used with erythromycin or ketoconazole.
Caused by decreased release of potassium |
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Term
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Definition
Cimetidine, ranitidine, nizatidine and famotidine. |
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Term
What are therapeutic used of H2 antagonists? |
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Definition
Acid reflux, ulcer and zollinger-syndrome |
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Term
What other drugs block the acid secretion by non H2-mechanism |
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Definition
Pirezepine: Blocks muscarinic receptor and Ach release from the paracine cells.
Misoprostol: prostaglandin analog
Omeprazole: Covalent inhibitor of H/K pump |
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Term
H2 antagonists side effects |
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Definition
Headache, dizziness, nausea.
Gynecomastia (men), glactorrhea (women) and loss of libido (cimetidine)
In elderly people it can cause slurred speech, delirium, and confusion.
Also, causes inhibition of CYP450 which affects oxidation oxidases such as warfarin, phenytoin, sulfonylureas and calcium channel blockers. |
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Term
What are platelet acting factors? (PAF) |
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Definition
These are synthesized in denove in response to antibodies reaction, collagens, thrombane.
The platelet acting factors are produced in platelets, neutrophil, monocytes, eiosinophils, vascular endothelium, and mast cells. |
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Term
Physiological actions of PAF |
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Definition
Potent vasoconstrictor, increases vacular permeability, potent stimulator of platelet aggregation. Involved in chemotaxis of neutrophils, monocytes and eosinophils. It is ulcerogenic and causes ovulation, implantation, and labor. |
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Term
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Definition
Implantation and pregnancy in-vitro is related with PAF and may be PAF release determines the best embryo for implantation.
PAF is also used in developing the medium for embryo and success rate is 50% |
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Term
Name the major subtype receptors for seratonin? |
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Definition
5HTID, 5HT2A, 5HT2C, 5HT3 AND 5HT4 |
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Term
PHYSIOLOGICAL ACTIONS OF SERATONIN. |
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Definition
FUNCTIONS ARE INVOLVED IN MOOD, SLEEP, BEHAVIOR, CONTROL OF BP, COGNITION, THERMOREGULATION, PAIN PERCEPTION, NEUROENDOCRINE EFFECTS AND SEXUAL BEHAVIORS.
CONTROLS BP BY WORKING BY SEPLANCHIC, RENAL, PULMONARY, AND CEREBRAL VASCULATURE |
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Term
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Definition
5HT2C AND 5HT2A ANTAGONIST
USED FOR PROPHYLACTIC MIGRAINES BY ANTAGONIZING THE VASODILATION NOT USED FOR ACUTE MIGRAINES. INHIBITS DIARRHEA ASSOCIATED WITH CARCINOID RELEASE
SIDE EFFECTS INCLUDE DIARRHEA, PAIN, HEARTBURN, NAUSEA, EUPHORIA, HALLUCINATIONS. |
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Term
KETANSERIN AND RITANSERINE |
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Definition
BLOCKS 5HT2A RECEPTOR. BLOCKS VASOCONSTRICTION AND PLATELET AGGREGATION
THIS IS USED FOR REYNAUDS PHENOMENON, HYPERTENSION, AND INTERMITTENT CLAUDICATION. |
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Term
ODANSTERONE AND GRANISTERONE |
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Definition
5HT2 ANTAGONIST. USED FOR NAUSEA AND VOMITINT CAUSED DUE TO CHEMOTHERAPY. SIDE EFFECTS INCLUDE NAUSEA AND VOMITING. |
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Term
TEGASEROD AND PUCALOPRIDE |
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Definition
IT IS 5HT4 AGONIST. USED FOR IRRATABLE BOWEL SYNDROME. SIDE EFFECTS ARE DIARRHEA |
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Term
What are the symptoms of ergot? |
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Definition
Vasoconstriction, gangrine in limbs, unintentional abortions, emesis, and severe nausea. |
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Term
Physiological affects of ergot alkaloids |
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Definition
Constrict veins and arteries by working on adrenergic and 5HT receptors. They are used to control breathing postpartum and post abortion. |
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Term
Name all the ergot alkaloids along with their therapeutic uses. |
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Definition
Ergotamine or dihydroergotamine; give for prodrome migraine headache.
Ergonovine; used for give after delivery to stop bleeding due to postpartum hemorrage.
Bromocryptine is give to the patients with pituatary tumor or accessive lactation due to DA agonist, dyskineasis with parkinson's, and acromegaly.
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Term
How prostanoids are synthesized |
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Definition
They are made by the action of cyclooxygenase (prostaglandine oxygenase) on arachnoid acid. |
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Term
Explain the physiological action of PGE, PGI, PGF and thromboxane |
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Definition
PGI dialates systemic and renal blood vessels, inhibit platelets aggregation and immune system.
PGE inhibits gastric secretion and induces pain, fever and GI mucus.
Thromboxane constricts system and renal blood vessels and induces platelet aggregation and immune system.
PGF constricts bronchiol and uterine smooth muscle.
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Term
What is used for reynaud's phenomenon? |
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Definition
PGE1 analogs are misopristol and rioprostil.
PGE2 are Enprostil and arbaprostil.
Dialate blood vessels |
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Term
List the names of PGI2, how they are administered and for what condition? |
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Definition
They are used for pulmonary hypertension.
epoprostenol, and flolan via IV
treprostinil, Remodulin via continuous subcutaneous.
Also, used for inhibition of platelet aggregation during dialysis and the analogs used for that are carbacyclin and illoprost. |
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Term
List PGF2 analogs and what are they used for ?
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Definition
Travoprost, lantanoprost and bimatoprost and they are used for glaucoma. |
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Term
List the PGE2 analog and what is used for? |
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Definition
Dinoprostpone, used during first and 2nd trimester abortion. Does it by causing uterine contractions and intravaginally is more effective with almost no side effects.
Another one is alprostadil used for congenital heart surgery in neonates. This one increases blood flow to the lungs and increases pulmonary and systemic heart surgery. |
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Term
What is 5-lipoxygenase and how is it activated? Where is it found? |
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Definition
It is formed by the action of 5-lipooxygenase on arachnoid acid. found in neutrophil, macrophages, monocytes, lungs, heart, spleen, lungs. it must attach to FLAP protein to be functional. |
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Term
What are primary metabolites of neutrophils and mast cells? |
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Definition
1. LTB4
2. LTC4, LTD4 and LTE4. |
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Term
List the functions of montelukast, zafirlukast, and zileuton |
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Definition
Montellukast and zafirlukast are LTC4 and LTE4 competitive antagonists. zileuton is 5-lo inhibitor.
It is used in an addition or as an alternative to corticosteroids or b2 agonists.
Side effects include nausea, headache and upset stomach |
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Term
What receptors does bradykinin works on? What are their functions? |
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Definition
The effects are mediated by two receptors B1 and B2.
B2 receptors are used in analgesia by stimulating the thin superficial layer of spinal cord, unmylenated nerves and sensory ganglia. Also, it vasodilate via NO release and direct vasoconstriction.
B1 causes inflammation by causing release of histamine from mast cells and edema by changing the permeability of the membrane. |
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Term
What are therapeutic effects of kinins? |
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Definition
Kininase II. Use to lower blood pressure by increasing flow to kidneys and increasing Na excretion. Also, increase bradykinin releases NO which causes vasodilation and decreases the blood pressure as well. |
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