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108 Cards in this Set
- Front
- Back
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Diphenhidramine
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First generation anti-histamine
Anticholinergic (dry mouth, hot dry skin, urinary retention, constipation, blurred vision) Sedating |
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Sedating first generation Antihistamines
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Diphenhydra
Prometh Hydroxyzine EtOH or other sedators compound the effects. |
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Loratidine
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Second generation antihistamine,
doesn't cross BBB sECOND GENS |
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Which antihistamine is eliminated by the kidney?
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Certrizine/Levocertrozine
give when liver is of concern |
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H1 receptor
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H1 receptor is linked to Gq protein ad stimulation increases the production of IP3/DAG
Found in smm mm, endothelium and brain Classic antihisamines block H1 decreases Bp, causes hives, edema, bronchospasm and itching-allergic reaction |
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H2 receptor
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H2 are linked to Gs and increase camp. H2 fond in heart and brain
have a significant role in gastric acid release |
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H3 and H4 receptors
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both are linked to Gi and decrease camp
3- brain and presynaptic where they decrease transmitter release 4- found on leukocytes and play in chemotaxis |
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second gen antihistamines metabolism
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all but Certrizine are metabolized by CYP3 and should not be taken w/ grapefruit.
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Cromalyn Sodium
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Blocks the release of histamine from mast cells,
used to treat asthma in chidren Nasal |
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Cimetidine
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H2 blocker- Decreases gastric acid release
Inhibits metabolism of lots of other drugs, has lots of drug interactions. High doses have an anti-androgen effect (boys turn to girls) |
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Asthma bronchodilators vs anti inflammatory
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Corticosteroids down are anti Inf
all above are bronchoD |
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Albuterol
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B2 agonist
Emergency- fast acting, used to treat asthma attack in progress less tolerance Can be used for mild |
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Salmeterol
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Long acting bonchoselective b2 agonist
effect takes about 20 min so its not effective in emergency, 12 hour effect, use corticosteroids to decrease tolerance Can be used as prophylaxis for long term bronchodilation such as surgery |
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S/E of B2 agonists
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Tremor, Tach, Dizzyness
you know, B2 stuff |
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Ipratroprium
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muscarinic antagonist used in COPD
causes bronchodilation Ipraytobreathe |
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theophyline
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rarely used as a bronchodilator.
inhibits breac of cAMP and adnosine receptor -- has a very narrow therapeutic range, anything that inhibits it smetabolism can cause toxic cardiac arrythmias. (ANTACIDS, CIMETIDINE) |
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Advantages to inhaled corticosteroids
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they are good as anti-inflammatories and derease the requirement for B antagonists
they have FEW side effects other than THRUSH which causes hoarsness |
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-lukasts
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block the LT receptors
decrease cold air/exercise asthma. Must be taken chronically. SE- sore throat, respiratory, sleepiness |
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Zileuton
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Blocks 5 lipox and decreases the synthesis of LT
decreases asthmatic reaction to NSAIDS and aspirin. |
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Omalizumab
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monoclonal antibody targeted to IgE preventing it from binding to MAst cells and Basophils
This is for SEVERE allergic asthma- not a routine drug. |
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Antacid drug interactions
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All antacids could potentially bind other drugs b/c they are divalent cations and will decrease their absorption
patients may not inform you they are taking these drugs |
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-prazoles
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PPIs- Pretty much all the same
irreversibly inhibit the proton bump at the GI parietal cell lasts up to 3 days with near total inhibition of gastric acid secretion grreat for ulcers, GERD, any time you want to decrease acid take on empty stomach SE- decreased Ca++ absorption= osteoporosis |
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Omeprazole
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Omeprazole, Esomeprazole, Lansoprazole inhibit
CYP2C19 and CYP3A4 so have significant drug interactions |
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Sucralfate
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Cryoprotective GI drug
- in stomach acid, poymerizes to form a sticky, viscous protective barrier in the ulcer crater causes constipatin- reacts w/ digitalis, pheny. |
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Misoprostol
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Cyroprotective drug not used anymore
CI in preggo b/c causes uterine contraction and abortion |
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Metoclopramide
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D2 receptor antagonist- to treate gastroparesis
increases ACH release to increase GI motility can cause diarrhea nad cramping but the major is a D2 ANTagonist effect whcih can cause parkinsons type syndromes- NO PREGGGGGOS |
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Muscarinic Antagonists
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Glycopyrollate and Bethanachol
- enhances motility and tone in the GI tract- post op ileus Has all the anti-muscarinic SE -sedation -ocular pressure increase -OD= confusion, agitation, sleeplesness for hours |
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Alosetron
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rarely used to treat IBS
many contraindications so rarely used KNOW IT IS A 5-HT3 receptor |
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Tegaserod
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selective serotonin 5HT4 partial
used to treat women with constipation |
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Odansetron
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Anti Nausea/emetic
Pts of chemotherapy, gastroenteritis, post anesthesia NOT for motion sickness (think histamine receptor) |
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Bulk fiber laxatives
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they all increase the bulk of feces by attracting water
Used to prevent or treat chronic constipation TAKE LOTS OF H2O |
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Osmotic Laxatives
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Mg hydroxide
Sodium Salts Lactulose ---All poorly absorbed salts or sugars that hold water int he intestine --- not for routine use |
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Lactulose
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poorly absorbed sugar that holds water in the intestines
Use it in Cirrhosis to clear NH3 from blood |
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Senna
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Plant extract ath acts on mucosa of the colon
8-10hrs of duration- very mild |
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Docusate Sodium
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Emulsifying agent that allows the water to penetrate the colonic contents and soften them
-efficacy is porr -stool softener |
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Lubiprostine
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CIC-2 Cl- channels
increases intestinal fluid secretin via activating these luminal cells of intestinal epithelium CAN BE TAKEN CHRONICALLY for chronic constipation |
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Alvimopam and Methylnaltrexone
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Opioid antagonist to prevent post op ileus
-"just recognize the name" |
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Loperamide
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Opioid antidiarrheal
Loperamide- doesn't get into brain Opioid analog that decreases peristalsis |
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Lomotil
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Opioid antidiarrheal
inhibits CHOLINERGIC receptors comb w/ atropine ---gets in the brain |
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Prolactin drugs
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Bromo and Cabergoline
used to treat porlacinomas that's it. |
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Somatropin and Somatrem
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for replacing GH in those that need it.
Adolescents that don't have GH!!!!!!!! Replacement therapy in adults strong anabolic actions ( but not the go to for anabolism) DOn't USEin EMERGENCY Situations |
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Mecasermin and Mecasermin rinfibate
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GH agonists but downstream of GH
Where you don't have appropriate GH trasnduction you can use these. they're not as good as actual GH |
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GH Antagonists
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Octreaotide and Manreotide- they're both Somatostatin AGONists
--- used to treat acromegaly and reduce acromegaly tumor size b/ direct antagonists can treat w/ other horomone systems and excess diarrhea b/c of GI inhibition effects |
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Somatostatin
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GH antagonist
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Pegvisomant
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antagonizes growth hormone receptor but doesn't reduce tumor size b/c blocks the negative feedback receptors as well so tumor pumps and dumps
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Leuprolide,
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GnRH agonist
a. Longer time to silence HPG axis. Initial surge. Because of this if you are trying to silence HPG axis to control testosterone etc. always give an anti-androgen like flutamine. Use to treat for ART (silence HPG axis to prevent LH surge before you want to it to take place) also for precosious puberty. |
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FSH vs LH Fertility Drug Schemes Men vs Women
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1. Men-start LH drug to stimulate testosterone, then give FSH for spermatogenesis.
2. Women-opposite. FSH first then one dose of LH to stimulate ovulation. 3. Many side effects-multiple birthing. MOST SERIOUS-in women-ovarian hyperstimulation syndrome!! |
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Steroid physiology
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a. All steroid drugs-work through nuclear receptors. Take longer to have an effect. Effects are longer lasting even after you withdraw from medication. Corticosteroids, mineralos, androgens, thyroid, etc. all work in same way.
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Anti Estrogens
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Tamoxifine
Teraminfine Raloxifene Clomifeene Fulvistrant |
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Tamoxifine
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SERM- Used in Tx and prophylaxis in female estrogen cancer
Agonist in bone Antagonist in breast cancer- can cause menopausal sx |
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Reloxafine
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SCERN
-only for osteoporosis in post-menopausal women -Agonist in breast -Antagonist in Bone/Uterus |
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Clomifiene
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Antagonist at the hypothalamus
feedback from endogenous estrogen- overstimulates overies GO TO DRUG FOR Fertility |
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Fulvistrant
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Pure antagonist
Full antagonist- binds to all the estrogen receptors- gives you menopausal symptoms |
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Aromatase inhibitors
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Anasterazole
inhibits estrogen irreversibly- Works for estrogen dependent Cancer Also used after tamoxifen failure |
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Will always give menopausal symptoms
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All antiestrogens
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Progesterone Drugs
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10. Progesterone
a. Typically in combo with estrogen. Can use in place of estrogen ifthey have contra indication for estrogen use. b. Mifepristone-glucocorticoid receptor blocker and antiprogestin i. Contraindicated in pregnancy. This is an abortion pill c. Danezol-used for endometriosis. Weak progestin. THAT’S ALL |
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How do contraceptives work?
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They inhibit the LH surge that would release an Egg from the ovary
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YAZ
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drospirenone and ethinyl estradiol
Mineralcorticoid antagonist with some progestin stuff --- Helps prevent symptoms of PMDD- the only one approved for this |
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contraceptives Absolute vs Relative contraindications
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Absolute- thromboembolic phenomena, estrogen-dependent neoplasm
Relative- Liver disease Drug Rxn: microsomal enzymes (St Johns Wart, phenytoin, carbemazepine, modafinil decrease effectiveness) |
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Hormone Replacement Therapy MUSTS
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a. Young girls-hypogonadal
b. Young women-premenopausal age who have removal of ovaries. c. Other guidelines i. Hysterectomy-don’t need to give progestin ii. If has uterus-give progestin also. |
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Androgens- actions
Side effects Drugs |
a. Virilizing and anabolic effects!!!! replacement and anabolic actions in the body
b. Use to restore anabolic action in the body, recoupe protein production in debilitated. c. Side effects-men-decrease sperm i. Women-masculinization d. Antiandrogens i. Flutamide ii. Finasteride-inhibit 5 alphano DHT. Prostate hair follicles are 2 targets. TERATOGENIC- |
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Insulin use
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both type I and II
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Ultra Short Acting Insulins
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Lispro
Aspart Glulisine |
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Short acting Insulins
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Novolin
Humulin Velosulin |
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INtermediate Acting Insulins
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Lente Humulin
Lente NPH Humulin |
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Long Acting Insulin
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Ultralente humulin
INsulin Glargine Detemir |
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Pre-mixed insulins
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Novolin, Humulin 70/30 etc
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Insulins that are IV compatable
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Ultrarapids and regular- others are not
they are clear in solution |
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Insulin Physiology
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Insulin causes uptake of glucose- expression of Glut receptors
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Sulfonylureas
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a. Cause direct release of insulin by closing K+ channel. Cuases unregulatedhypoglycemia!!
b. Weight gain!! c. These are not nearly as bad in second generation. d. SULFA DRUGS |
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Meglitinides
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a. Much shorter half life-very small chance of causing hypoglycemia.
b. Metformin-DOC i. This is why DOC: Reduces macrovascular events. No effect on weight. ii. Adverse-Diarrhea and Lactic Acidosis!!!!!!! This is the one reason (lactic acidosis) why you wouldn’t prescribe it. iii. Renal, hepatic, hypoxia (COPD, CHF)-don’t give it |
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Thiazoleindiones (TZD)
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a. PPAR gamma-target tissue insulin like effects. nuclear receptor. Lower insulin resistance. Problem-EDEMA and this can be very bad. Don’t give to CHF patient where you’ll make them worse. Roseglitazone-black box-MI patients.
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Alpha Glucosidase
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Flatulence
a. Inhibit digestion of complex carbs. b. FLATULENCE |
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Incretins- exenatide liraglutide
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a. Resistance to DPPIV inactivation-INJECTION.
b. First drug that promote weight loss. They are fuller faster. c. Problem with this and next set-pancreatitis. |
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Gliptins
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a. DPP IV inhibitors.
b. Potentiate the incretin hormones. They don’t have weight loss. No weight gain but they don’t cause weight loss. |
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Pramlintide
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only drug for Type I and Type II.
a. Only as adjunct to insulin therapy. Can’t give as starting drug unless already taking insulin. Regulates postprandial glucose. Short action, injection. |
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Bromocriptine
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DA agonist. This inhibits Sympathetic surge in the morning to help compensate for hypoglycemic state. Prevents gluconeogenesis in that way. That’s all you need to know.
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Hyperglycemic/INsulinoma
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a. Glucagon-emergency rescue to mobilize hepatic glucose. No glycogen-worthless.
b. Diazoxide-insulinoma |
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Insulin workshop 4 points
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a. Dosing regimens-Type I injectable-make insulin profile and then you eat food to fill it
b. Pump-program in and say how much you need to cover what you’re about to eat. c. Rapid acting-basal level through the day and bolus insulin d. Hypoglycemia-stringent standards to keep HbA1c below 7. Some patients can’t handle. Don’t want to go below 6 in some-deliterious and may kill patients. |
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Uterine Relaxants
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a. He’ll have to give something that clues us in to what these are.
b. Magnesium sulfate-IV only c. Nifedipine-oral, Ca channel blocker d. Indomethacin-oral, inhibits PG production. Side effect-partial closure of patent ductus arteriosis e. Progesterone-prophylaxis only f. Nitro-emergency only g. Ethanol-only if nothing else |
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Oxytocin
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a. Oxytocin-DOC induce labor at term. Only then
i. Postpartum hemorrhage also. Stimulate milk letdown ii. Problem-water intoxication, uterine rupture, fetal distress. |
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Ergots- Uterine Contraction
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Uterine Contractions
c. Ergots-only for postpartum after delivery of placenta i. Nonphysiological strong contraction of uterus |
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Carboprost
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prostaglandin uterine contractor
used to induce abortion in the 13-20th week - bad in pt w/ asthma, HTN, Anemia, jaundice epilepsy Massive GI side effects |
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Dinoprostone
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e. Dinoprostone-not specified for postpartum hemorrhage. For abortion and cervical ripening.
Massive GI side effects |
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Hydrocortisone
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a. Hydrocortisone, cortisone equal effects. used for replacement therapy.
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Predinsone
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b. Prednisone, prednisolone-more glucocorticoid activity than mineralocorticoid.
i. First line-antifinlammatory long term |
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Fluticasone
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anti-inflammatory corticosteroid
i. Fluticasone-inhaled, intranasal. |
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Dexamethasone
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ii. Dexamethasone-cerebral edema, HPA suppression test to diagnose cushings.
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Addison pt or pts on long term glucocorticoid antiinflammatories
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d. Addison’s patient or long term glucocorticoid antifinlammatory-suppressing their HPA axis. They need increased level of glucocorticoids for any stress in their life. Minor-couple pills more, major-10x.
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Corticosteroid Therapeutic guidelines
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i. Want to minimize these as much as we can. Alternate day dosing, locally if possible, topicals, little as you can, this will help reduce HPA axis depression.
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Iatrogenic Renal Insufficiency
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After more than 1-2wks of therapy the HPA axis becomes depressed, if stopped abruptly adrenal insufficiency will occur
S |
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Corticosteroid therapy SE
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Acne, truncal obesity, increased apetie, buffalo hump , moon face, dysmenorrheal, skin atrophy, easy bruising
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Corticosteroid CNS side effects
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acute treatment with corticosteroids can case restlessness and insomnia, CNS effects occur rapidly
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Corticosteroid use Side Effects/Contraindicatiosn
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Bacterial infections, DM, Osteoporosis, heart disease, hypertension, systemic cviral infectionss receiving immunosuppresion
TERATOGENIC in pregnancy |
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Addison's or corticosteroid replacemnt therapy side-effects
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NO contraindications in pt with adrenal insufficiency
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Mifepristion and Spironolactone
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Corticosteroids
Spironolactone for hyperaldosteronism |
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Levothyroxine
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a. Levothyroxine-DOC for long term throid replacement therapy
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Liotheyronine
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b. Liothyronine-to get them to euthyroid state
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Thyroid Drug interactions
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Read the list- it's friggin long- serously read it
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Medical hyperthyroidism and tx
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e. Hyperthyroidism-if hypothyroid gets too much. How do you treat medical hyperthyroidism?
i. Methimazole and PTU. 1. Methimazole-DOC for Grave’s disease. Inhibit synthesis of TH. 2. 2 instances where you will use PTU instead of methimazole-pregnancy and allergy to methimazole. 3. Granulocytopenia, agranulocytosis-side effects |
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Iodine/radioactive
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Hyperthyroidism
ii. Iodide-not effective. Short. Effective prior to surgery to prevent thyroid storm when you cut into the gland. radioactive- iii. Radioactive-ablate the gland in cases where they can’t have surgery or mop up residual |
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Propanolol
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just to block symptoms of hyperthyroid
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Terapajireu
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d. Terapajireu-PTH use intermittently once a day moves from bad effect on bone to positive. ANABOLIC DRUG IN THIS CATEGORY-CAUSES BOnE GROWTH.
i. Because of intermittent treatment schedule |
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Denosumab
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Used in Osteoporosis
e. Denosumab-RANK ligand inhibitor. i. Going to inhibit osteoclasts |
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Bisphosphonates
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DOC for osteoporosis. Always go here!!!
i. Make sure you know which are IV and oral. Oral ones you have to have nasty dosing regimen-empty stomach, remain upright, blah blah. If patient with GERD-can’t give oral. If oral and IV-going to go with IV. 1. IV causes renal toxicity if given too fast. if renal patient, don’t want to go IV. 2. Know which are used. Others are used off label, those might be there as distractors |
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Citacalset
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Osteoporosis
didn’t talk about it-inhibits PTH release. |
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IV osteoporosis drugs
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find them
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Oral Osteoporosis drugs
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find them
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