Drugs

Question 1

Motion sickness drugs

Answer 1

Want anticholinergic (muscarinic receptor
antagonist)
– Diphenhydramine (Benadryl®) – Dimenhydrinate (Dramamine®) – Meclizine (Bonine®) – Scopolamine (Transderm Scop®)

Question 2

Drugs to treat drug induced nausea/vomiting:

Dopamine receptor blockers

Answer 2

– Promethazine (Phenergan®)
– Prochlorperazine (Compazine®)
– Trimethobenzamide (Tigan®)

Question 3

Drugs to treat drug induced nausea/vomiting:

Serotonin receptor blockers

Answer 3

– Ondansetron (Zofran®)
– Dolasetron (Anzemet®)

Question 4

Drug induced nausea/vomiting treatment:

Blocks both seratonin AND Dopamine

Answer 4

Metoclopramide (Reglan®)

Question 5

Non sedating anti histamines

Answer 5

Cant use for PD, cant cross BBB

Terfenadine (Seldane), Astemizole (Hismanal), Fexofenadine (Allegra), Loratadine (Claritin), Cetirizine (Zyrtec)

Question 6

CYP- 1A2 enzyme substrares, inhibitors, inducers

Answer 6

Substrates: Tacrine, Amitriptyline, Theophylline

Enz inhibitors:
Erythromycin, ciprofloxacin

Enz inducers: Carbamazepine, Rifampin, Tobacco

Question 7

CYP-2C9 enzyme substrates, inhibitors, inducers

Answer 7

Substrates:
Warfarin
Tolbutamide
Phenytoin

Inhibitors:
Paroxitene, Fluoxetine
Metronidazole*
Fluconazole*

Inducers:
Phenobarbital
Rifampin

Question 8

CYP-3A4 enzyme substrates, inhibitors, inducers

Answer 8

Substrates:
Lovastatin, Simvastatin Terfenadine (seldane), Astemizole (hismanal)
Estrogen, Progestins

Inhibitors:
Erythromycin* Clarithromycin*
Grape Fruit Juice
(Taking these will increase seldane and hismanal levels))

Inducers:

Carbamazepine
Rifampin
St John’s Wort (

Question 9

H2 receptor blockers: uses, examples

Answer 9

Treatment of GI Ulcers

Cimetidine (Tagamet®) Ranitidine (Zantac®) **
Famotidine (Pepcid®)+

Note: ranitidine manufacturing had carcinogens? So now zanrac

Question 10

Other non-H2 treatments for GERD

Answer 10

Can use anti-ACH drugs like Atropine, Pirenzepine, but the side effects are reeeally bad and last all day

Prostaglandin agonist: Misoprostol (Cytotec)
(DO NOT use for pregnant patients, stimulates uterine contractions

Protein pump inhibitors (PPI):
Omeprazole (Prilosec®) Antacids
Lansoprazole (Prevacid®)
“The purple pill” -Esomeprazole (Nexium®)

Note PPIs don’t prevent recurrence, so use Clarithromycin (Biaxin) and Amoxoxillin (trimox) to target H. pylori

Question 11

Protein pump inhibitors (PPI):

Answer 11

Omeprazole (Prilosec®) Antacids
Lansoprazole (Prevacid®)
“The purple pill” -Esomeprazole (Nexium®)

Question 12

Prostaglandin agonist:

Answer 12

Misoprostol (Cytotec ®)
Diclofenac/misoprostol (Arthrotec ®)

(DO NOT use for pregnant patients, stimulates uterine contractions

Question 13

What do the adrenal glands release? What “axes” are these a part of?

Answer 13

Glucocorticoids (cortisol), part of a feedback loop with hypothalamus—> pituitary—>ACTH—>adrenal cortex—> cortisi

Mineralcorticoids (aldosterone), part of the Renin-Angiotensin acis

Question 14

Do you use glucocorticoids for immediate treatment of anaphylaxis? Why or why not?

Answer 14

No bc cortisol is a steroid—> its MOA is on transcription—> takes time for effect to set in

Question 15

How can you treat CHF by affecting the RAA system?

Answer 15

Aldosterone will increase water and sodium retention

ACE1 inhibitors lead vasodilation and less aldosterone, which leads to more water and sodium excreted. Good for CHF patients

Question 16

General effects of glucocorticoids, and major examples

Answer 16

• main effect: control carb metabolism. More potent glucocorticoid= more glycogen deposition in liver, more anti-inflammatory
• can enhance catecholamines (epinephrine, albuterol at B2 receptor)
• more fat deposition around face, back (Cushing’s syndrome)
• lower vit D activity, lower calcium absorption, more bone catabopism (bad, could accelerate osteoperosis)
• Acute Adrenal Crisis
• anti inflammatoey means immunosuppression (less lymphcytes, dampened response, less cytokine released, lower COX release)
• more RBCs
• glucocorticoids + NSAIDS = stomach ulcer
• stimulate lung development in fetus, give to mom at premature birth

Examples: aldosterone, cortisone, hydroxcortisone, prednisone, triamcimopome

Most potent: dexamethasone, betamethasone

Question 17

What is Acute Adrenal Crisis?

Answer 17

If you’re on Cortisol for 2 weeks or more, you stop producing endogenous cortisol—> can lead to rapid hypoglycemia, loss of consciousness

Question 18

Mineralcorticoid examples

Answer 18

Natural: 11-deoxycorticosterone
Aldosterone

Many glucocorticoids also have mineral effects (cortisone, hydrocor, prenisolone)

Question 19

Structures and functions of corticosteroids

Answer 19

• no hydoxyl 17, no glucocorticoid activity (present means yes)
• undaturated 2x bond btw C1 and 2, increase glucocorticoid/anti-inflammation
• Dexamethasone has 2x bond a C1=C2, halogenation at C9, methylation at C16–> the most potent glucocorticoid

Question 20

Major diseases treated w glucocorticoids

Answer 20

GI diseases like UC, crohn’s, celiac

Organ transplants

Lupus, sarcoidosis

Contact detmatitis and lichen planus, tho mainly as an ointment

Arthritis: Rheymatoid (short term), osteoarthritis (direct koint injection

Decrease swelling after wisdom tooth (Medrol)