S3M2 Pharmacology Beevers Autocoids/ai Drugs

Front 1

What is the MOA for Triptans?

What is the MOA for Glucocorticoids?

Back 1

Triptans are 5-HT AGONISTS

GC's act in the nucleus as Transcription factors

Front 2

What does Histamine do? (4 things)

Back 2

1.) Allergic and inflammatory rxn
2.) Gastric acid secretion
3.) NT
4.) Chemotactic agent for WBCs

Front 3

Histamine receptors are G-coupled receptors:

1.)H1
2.)H2
3.)H3
4.)H4

Back 3

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

Front 4

Histamine receptor functions:

1.) H1
2.)H2
3.)H3
4.)H4

Back 4

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

Front 5

These drugs PHYSIOLOGICALLY inhibit histamine by reducing degranulation of histamine release caused by allergy.

Back 5

-Cromolyn
-Nedocromic
-B2 Agonist (albuterol/salmeterol)

Front 6

1st Generation H1-antagonist drugs.

-MOA?
-CI
-Drug names?

Back 6

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

CI in pregnancy

cyclizine
cyproheptadine
dimenhydrinate
diphenhydramine
Meclizine
Promethazine

Front 7

Cyproheptadine

Back 7

H-1 antagonist
(also blocks serotonin 5-HT)

Tx: Carcinoid Tumor

Front 8

Dimenhydrinate

Back 8

H-1 antagonist

Tx: Motion sickness

Front 9

Diphenhydramine

Back 9

H-1 antagonist
(also has anti-muscarinic action so anti-parkinson)

-Local anesthetic with Promethazine

-PREVENTION of motion sickness

Front 10

Promethazine

Back 10

H-1 antagonist
(also blocks a-receptors and can cause orthostatic hypotension)

-Local anesthetic with diphenhydramine

-PREVENTION of motion sickness

Front 11

2nd Generation H-1 Antagonists?

Back 11

THEY DO NOT enter the CNS=no sedation

LONGER duration of action12-24h

C: cetirizine
F: Fexofenedine
L: Loratadine

Front 12

H-2 Antagonists

"2 tidines"

-Can you take antacids with these?

Back 12

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

Front 13

This NT is fromed from Tryptophan and is found in :
1.)Enterochromaffin cells of the GI
2.) Platelets
3.) Raphe nucleus of brain

Back 13

Serotonin (5-HT)

Front 14

Serotonin is involved in:

Back 14

-5-HT is precursor of melatonin
-Vomit reflex
-^^^ peristalsis via 5-HT 2
-stimulates pain and itching

Front 15

Does serotonin cause vasocontriction or vasodilation?

Back 15

BOTH
-Vasocontriction in pulmonary vessels
-vasodilation in skeletal/coronary vessels

Front 16

What G proteins are associated with:

5HT1

5HT2

Back 16

5HT1: Gi: decreases cAMP

5HT2: Gq: IP3/DAG ^^ Ca++

Front 17

Buspirone

Back 17

Serotonin AGONIST
Tx: GAD

Front 18

Ergonovine

Back 18

Serotonin AGONIST
Tx: control post partum bleeding by contraction of uterus

Dx: Variant Angina (angina at rest)

Front 19

Ergotamine

Back 19

Serotonin AGONIST

USE WITH CAFFEINE!!
@ first sign of migraine pain only;
POTENT vasocontrictor

Front 20

Triptans are:
1.) Receptor?
2.) Drugs?
3.) Tx?

Back 20

5HT1-B and 5HT 1-D Agonists

Almo, Nora, Suma

DOC for migraine headaches

Front 21

Vitamin is converted to a cofactor used in transamination (ALT, AST)?

Back 21

Vitamin B6 (pyridoxine)
-->Req. for Niacin syn from Tryptophan

Front 22

How to triptans work?
(Almo, nora, Suma)?

Explain Serotonin Storm.

Back 22

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.

Front 23

5-HT ANTAGONISTS are...

Back 23

1.)cyproheptadine (Carinoid tumor)
2.) Ondansetron- 5HT3 (N&V)
3.) Ritanserin (reduce thromboxane and alters bleeding time)
4.) Phenoxybenzamine
5.) Phenylthiosine and Butyrophenoms

Front 24

Alprostadil

Back 24

-Erectile dysfunction
-Maintain patent ductus arteriosus

**Prolonged erection and penis pain

Front 25

Carboprost

Back 25

2nd Trimester abortion
and control PP bleeding

Front 26

Dinoprostone

Back 26

2nd Trimester abortion
and Ripens cervix for labor

-Also removal of hydatidiform mole

Front 27

Epoprostenol-->Must be continuous IV

Back 27

Tx: Primary pulmonary hypertension and can delay the need for lung/heart transplant

Front 28

Latanoprost

Back 28

Prodrug eyedrops
Tx: Glaucoma

Front 29

Misoprostol

Back 29

Tx: of NSAID induced Peptic ulcers

Used with diclofenac to treat upper GI ulcers

Front 30

1.) Which Eicosanoid inhibitors block Luekotriene receptors?

2.) Which Eicosanoid inhibitor works directly on LOX enzyme?

Back 30

1.) Zafirlukast and Montelukast

2.) Zileuton "Zileuton-LoX"

Front 31

What do Glucocorticoids block?

Back 31

They block Phoshoplipase and Cox 2

Front 32

What do NSAIDS do?

Back 32

1.) Anti-inflammatory--> inhibit TXA2 and PG synthesis
2.) Analgesic (pain killer)
3.) Anti-pyretic

*** No effect on immune system

Front 33

This group of drugs are
-Well absorbed
-Highly metabolized and excreted by the KIDNEY!!!
-Most reversibly and competatively inhibit Cox1/Cox2 enzymes

Back 33

NSAIDS

Front 34

Salicylic Acids (aspirin, sulfosalazine)

They inhibit Cox pathway and decrease PG synthesis

What are they Adverse effects?

Back 34

-Tinnitis
-Errosive gastritis
-Severe hepatic injury

CI: pregnancy and viral illness in children

Front 35

Sulfosalazine

Back 35

Tx: Ulcerative colitis and chrohns disease

Front 36

What are the clinical uses of aspirin?

Back 36

Aspirine IRREVERSIBLY binds and inhibits Cox
-Anti-platelet (after MI)
-Anti-pyretic
-Analgesic
-Anti-inflammatory

Front 37

Type of NSAIDS:
Proprionic acid derivatives

Back 37

1.) Flubiprofen
2.) Ibuprofen-->Closes patent ductus arteriosus
Tx: osteoarthritis and dental pain

3.) Naproxen: single enantiomer

4.) Oxaprozin: Gout

Front 38

Types of NSAIDS
Acetic acid derivatives

Back 38

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

Front 39

Indomethacin

Back 39

Non-selective Cox but also inhibits PLA and PLC

Tx: closes patent ductus arteriosus

CI w/ probenecid and during 3rd trimester

Front 40

Oxicams

Back 40

1.) Meloxicam is MOSTLY Cox-2
Tx: OSTEOARTHRITIS

2.) Piroxicam: Non-selective COX
inbits WBC migration and decreases oxygen radicals
**9x ulcers and bleeding

Front 41

Celecoxib

Back 41

HIGHLY selective for cox 2 (just like meloxicam)
**does NOT affect platelet fxn and reduced risk of GI ulcers
CI with preg and warfarin

Front 42

Acetaminophen

CI w/ alcohol

Back 42

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

Front 43

Glucocorticoid MOA

Back 43

GC act on GC receptors--> go into nucleus as a TF and directly binds to GC response element

Front 44

This drug is
1.) anti-inflammatory
2.) immune suppressant
3.) fetal lung development

Back 44

Glucocorticoids

Front 45

What do Glucocorticoids cure?

precautions?

Back 45

They cure adrenal insufficiency (addisons)

Must ween off the drug slowly

Front 46

What are the short acting Glucocorticoids?

Back 46

CHMPP
Cortisone
Hydro-cortisone
Methyl prednisolone
Prednisolone
Prednisone

Front 47

What are the long acting glucocorticoids?

Back 47

Betamethasone

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