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47 Cards in this Set

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What is the MOA for Triptans?

What is the MOA for Glucocorticoids?
Triptans are 5-HT AGONISTS

GC's act in the nucleus as Transcription factors
What does Histamine do? (4 things)
1.) Allergic and inflammatory rxn
2.) Gastric acid secretion
3.) NT
4.) Chemotactic agent for WBCs
Histamine receptors are G-coupled receptors:

1.)H1
2.)H2
3.)H3
4.)H4
1.) H1 is Gq: IP3/Dag: ^Ca++
Smooth muscle, endothelium, POST-synaptic in the brain

2.) H2 is Gs: ^cAMP
Gastric mucosa, cardiac muscle, POST-synaptic

3.) H3 is Gi: decrease cAMP
Myenteric plexus, PRE-synaptic in the brain

4.) H4 is Gi: decrease cAMP
Leukocyte migration
Histamine receptor functions:

1.) H1
2.)H2
3.)H3
4.)H4
1.) H1: causes uterus contraction, bronchoconstriction, peristalsis, Urticaria, Vasodilation and hypotension

H2 causes increase pepsin, gastric acid, IF and also increases contractility of the heart

H3: Auto-receptor
H4: Chemotactic agent for WBCs
These drugs PHYSIOLOGICALLY inhibit histamine by reducing degranulation of histamine release caused by allergy.
-Cromolyn
-Nedocromic
-B2 Agonist (albuterol/salmeterol)
1st Generation H1-antagonist drugs.

-MOA?
-CI
-Drug names?
MOA: competative inhibition of H-1 receptors/ Can enter CNS and cause sedation

CI in pregnancy

cyclizine
cyproheptadine
dimenhydrinate
diphenhydramine
Meclizine
Promethazine
Cyproheptadine
H-1 antagonist
(also blocks serotonin 5-HT)

Tx: Carcinoid Tumor
Dimenhydrinate
H-1 antagonist

Tx: Motion sickness
Diphenhydramine
H-1 antagonist
(also has anti-muscarinic action so anti-parkinson)

-Local anesthetic with Promethazine

-PREVENTION of motion sickness
Promethazine
H-1 antagonist
(also blocks a-receptors and can cause orthostatic hypotension)

-Local anesthetic with diphenhydramine

-PREVENTION of motion sickness
2nd Generation H-1 Antagonists?
THEY DO NOT enter the CNS=no sedation

LONGER duration of action12-24h

C: cetirizine
F: Fexofenedine
L: Loratadine
H-2 Antagonists

"2 tidines"

-Can you take antacids with these?
1.)Famo
2.)Nizo
3.)Rani
4.)Cimetidine

Tx: Peptic Ulcers NOT caused by NSAIDS
--In that case you would use PP inhibitors or misoprostol

No antacids!!! B/c they prevent the absorption of the H-2 antagonists
This NT is fromed from Tryptophan and is found in :
1.)Enterochromaffin cells of the GI
2.) Platelets
3.) Raphe nucleus of brain
Serotonin (5-HT)
Serotonin is involved in:
-5-HT is precursor of melatonin
-Vomit reflex
-^^^ peristalsis via 5-HT 2
-stimulates pain and itching
Does serotonin cause vasocontriction or vasodilation?
BOTH
-Vasocontriction in pulmonary vessels
-vasodilation in skeletal/coronary vessels
What G proteins are associated with:

5HT1

5HT2
5HT1: Gi: decreases cAMP

5HT2: Gq: IP3/DAG ^^ Ca++
Buspirone
Serotonin AGONIST
Tx: GAD
Ergonovine
Serotonin AGONIST
Tx: control post partum bleeding by contraction of uterus

Dx: Variant Angina (angina at rest)
Ergotamine
Serotonin AGONIST

USE WITH CAFFEINE!!
@ first sign of migraine pain only;
POTENT vasocontrictor
Triptans are:
1.) Receptor?
2.) Drugs?
3.) Tx?
5HT1-B and 5HT 1-D Agonists

Almo, Nora, Suma

DOC for migraine headaches
Vitamin is converted to a cofactor used in transamination (ALT, AST)?
Vitamin B6 (pyridoxine)
-->Req. for Niacin syn from Tryptophan
How to triptans work?
(Almo, nora, Suma)?

Explain Serotonin Storm.
They cause vasocontriction of cerebral vessels AND INHIBIT THE RELEASE OF VASODILATION PEPTIDES.

You CANNOT give 5-HT agonists in conjunction with SSRI's, MOAI's or other 5-HT agonists b/c you will cause serotonin storm.
5-HT ANTAGONISTS are...
1.)cyproheptadine (Carinoid tumor)
2.) Ondansetron- 5HT3 (N&V)
3.) Ritanserin (reduce thromboxane and alters bleeding time)
4.) Phenoxybenzamine
5.) Phenylthiosine and Butyrophenoms
Alprostadil
-Erectile dysfunction
-Maintain patent ductus arteriosus

**Prolonged erection and penis pain
Carboprost
2nd Trimester abortion
and control PP bleeding
Dinoprostone
2nd Trimester abortion
and Ripens cervix for labor

-Also removal of hydatidiform mole
Epoprostenol-->Must be continuous IV
Tx: Primary pulmonary hypertension and can delay the need for lung/heart transplant
Latanoprost
Prodrug eyedrops
Tx: Glaucoma
Misoprostol
Tx: of NSAID induced Peptic ulcers

Used with diclofenac to treat upper GI ulcers
1.) Which Eicosanoid inhibitors block Luekotriene receptors?

2.) Which Eicosanoid inhibitor works directly on LOX enzyme?
1.) Zafirlukast and Montelukast

2.) Zileuton "Zileuton-LoX"
What do Glucocorticoids block?
They block Phoshoplipase and Cox 2
What do NSAIDS do?
1.) Anti-inflammatory--> inhibit TXA2 and PG synthesis
2.) Analgesic (pain killer)
3.) Anti-pyretic

*** No effect on immune system
This group of drugs are
-Well absorbed
-Highly metabolized and excreted by the KIDNEY!!!
-Most reversibly and competatively inhibit Cox1/Cox2 enzymes
NSAIDS
Salicylic Acids (aspirin, sulfosalazine)

They inhibit Cox pathway and decrease PG synthesis

What are they Adverse effects?
-Tinnitis
-Errosive gastritis
-Severe hepatic injury

CI: pregnancy and viral illness in children
Sulfosalazine
Tx: Ulcerative colitis and chrohns disease
What are the clinical uses of aspirin?
Aspirine IRREVERSIBLY binds and inhibits Cox
-Anti-platelet (after MI)
-Anti-pyretic
-Analgesic
-Anti-inflammatory
Type of NSAIDS:
Proprionic acid derivatives
1.) Flubiprofen
2.) Ibuprofen-->Closes patent ductus arteriosus
Tx: osteoarthritis and dental pain

3.) Naproxen: single enantiomer

4.) Oxaprozin: Gout
Types of NSAIDS
Acetic acid derivatives
1.) Diclofenac
Inhibits BOTH COX(1/2) and LOX
Tx: Upper GI ulcers with misoprostol

2.) Ketorolac- Replaces morphine; great analgesic
ADV-->60% of the drug is wholly excreted by kidney; can cause renal toxicity

3.) Sulindac: Tx: Familial Adenomatus polyposis and MAY prevent breast, prostate and colon cancer
Indomethacin
Non-selective Cox but also inhibits PLA and PLC

Tx: closes patent ductus arteriosus

CI w/ probenecid and during 3rd trimester
Oxicams
1.) Meloxicam is MOSTLY Cox-2
Tx: OSTEOARTHRITIS

2.) Piroxicam: Non-selective COX
inbits WBC migration and decreases oxygen radicals
**9x ulcers and bleeding
Celecoxib
HIGHLY selective for cox 2 (just like meloxicam)
**does NOT affect platelet fxn and reduced risk of GI ulcers
CI with preg and warfarin
Acetaminophen

CI w/ alcohol
NOT NSAID
NOT used for anti-inflammatory

Potent inhibitor of Cox enzymes in the CNS
-Analgesic
-Antipyretic

preferred over aspirin if pt. is hemophiliac, asthmatic, or has ulcers
Glucocorticoid MOA
GC act on GC receptors--> go into nucleus as a TF and directly binds to GC response element
This drug is
1.) anti-inflammatory
2.) immune suppressant
3.) fetal lung development
Glucocorticoids
What do Glucocorticoids cure?

precautions?
They cure adrenal insufficiency (addisons)

Must ween off the drug slowly
What are the short acting Glucocorticoids?
CHMPP
Cortisone
Hydro-cortisone
Methyl prednisolone
Prednisolone
Prednisone
What are the long acting glucocorticoids?
Betamethasone

Dexamethasone-->used to Dx: cushings or ectopic ACTH secreting tumor