Exam 4 Flashcards
3 Short-Medium acting Glucocorticoids
Hydrocortisone
Prednisone
Methylprednisolone
Intermediate Acting Glucocorticoid
Triamcinolone
Long acting Glucocorticoid
Dexamethasone
2 Glucocorticoid synthesis inhibitors/antagonists
Metyrapone
Ketoconazole
Mineralocorticoid agonist
Fludrocortisone
Mineralocorticoid antagonist
Spironolactione
4 Glucocorticoids Used to Treat Asthma
Prednisone, Methylprednisolone, Triamcinolone, Dexamethasone
All the ones we know minus hydrocortisone
Steroid Tx for Cerebral Edema
Prednisone
Steroid Tx for Bacterial Meningitis
Dexamethasone
Steroid Tx for Collagen Disorders (SLE, Polymyalgia rheumatica, myositis)
Prednisone, Methylprednisolone, Triamcinolone, Dexamethasone
All the ones we know minus hydrocortisone, same as for asthma
Steroid Tx for Hematological Disorders (Autoimmune hemolytic anemia, Thrombocytopenia purpura)
Prednisone, Triamcinolone, Dexamethasone
Asthma/Collagen drugs minus Methylprednisone
Steroid Tx for Idiopathic Nephrotic Syndrome
Methylprednisolone
Steroid Tx for pulmonary sarcoidosis
Prednisone
Steroid Tx for Respiratory Distress Syndrome in the premature neonate
Dexamethasone
Describe Hydrocortisone, Prednisone, Triamcinolone, and Dexamethasone in terms of their Anti-inflammatory properties and mineralocorticoid potency.
Hydrocortisone has low AI potency and High mineralocorticoid potency.
Prednisone has medium AI potency and Moderate mineralocorticoid potency.
Triamcinolone has Medium AI potency and no mineralocorticoid potency
Dexamethasone has very high AI potency and no mineralocorticoid potency.
Fludrocortisone
Mineralocorticoid agonist
Has both mineral/glucocorticoid properties.
Tx for adrenocortical insufficiency associated with mineralocorticoid deficiency.
Metyrapone
Inhibitor of cortisol and aldosterone synthesis
Inhibits CYP11B1
Cushing’s Tx
Ketoconazole
Blocks all steroid synthesis by inhibiting CYP17 and at higher concentrations CYP11A1.
Most effective inhibitor in tx of Cushing’s
Typically used before Metyrapone with Metyrapone added if necessary (they exhibit synergism)
Also an antifungal agent
Spironolactone
Mineralocorticoid antagonist
Tx for hyperaldosteronism
Given before adrenal adenoma surgery to normalize potassium.
Cosyntropin
Synthetic ACTH
Used to test adrenal function.
Aspirin
Cyclooxygenase inhibitor
Suppresses of Thromboxane, which is a proaggregatory substance produced by platelets.
The effect is irreversible and lasts as long as the affected platelet is alive.
Used to prevent MI, ischemic strokes.
Used after CABG to prevent graft occlusion.
160-325 mg/day is antiplatelet dose
GI side effects
May effect hemostasis in surgery (more bleeding)
May cause problems in pregnancy.
Heparin
Antigoagulant via binding to Lysine residues of Antithrombin III (a protease inhibitor) and accelerating its activity.
AT III inactivates Xa and Thrombin, preventing conversion of fibrinogen to fibrin.
Also inhibits platelet function (can cause thrombocytopenia)
Its a mix of mucopolysaccharides that is synthesized in mast cells, especially in the lungs.
Administered by IV and works rapidly.
Used to treat MI, during heart surgery with extracorporeal circulation, and to keep CV catheters patent.
Better than oral anticoagulants during pregnancy.
Usage monitored by PTT, APTT.
Quite a few side effects…
Antidote to OD is Protamine sulfate.
Protamine sulfate
Strongly basic proteins originally harvested from fish sperm
Binds to Heparin due to its positive charge and reverses its effect immediately.
Lasts about 2 hours.
Too much can have anticoagulant activity of its own.
Less effective at inhibiting low molecular weight heparin.
Side effects include transient hypotension and allergic reactions (fish allergy?)
Warfarin
Oral anticoagulant.
Blocks Vitamin K in the liver, inhibiting the synthesis of clotting factors.
Works slower than heparin because clotting factors already in blood are unaffected.
Used to prevent thromboembolism in patients with chronic conditions (A fib, prosthetic valves, indwelling venous catheters, etc.)
Also used as part of chemo for some cancer treatments.
Risk of bleeding, hypertension, soft tissue necrosis, GI problems.
Dont give it to pregnant patients. It will cross the placenta and severely mess up the fetus. Use heparin instead if necessary.
Aspirin may intensify its affect.
Corticosteroids or too much vitamin K may decrease its affect.
Too much can be reversed with Vitamin K and FFP.
Lepirudin
Thrombin inhibitor
Yeast polypeptide
IV injected, very short halflife.
Used as an anticoagulant in patients with heparin-induced thrombocytopenia.
Side effects include hypersensitivities, bleeding, may affect fetus.
No antidote for OD.
Alteplase
tPA
Serine protease
Activates fibrin bound plasminogen to plasmin.
Can be reversed with Aminocaproic acid
Aminocaproic acid
Reverses alteplase (tPA)
Factor VIII
Antihemophilic factor
Treats hemophilia A, which is a factor VIII deficiency
Clopidogrel
Oral antiplatelet
Inhibits platelet aggregation
Inhibits the irreversible binding of ADP to the ADP receptor
Platelets exposed to clopidogrel are thus effected for their entire lifespan.
Used to prevent MI, stroke in high risk patients
Dipyramidamole
Blocks platelet adhesion to the subendothelium by inhibiting phosphodiesterase, increasing cAMP
Tirofiban
Antagonist of the platelet glycopritein IIb/IIIa receptor.
Inhibits platelet aggregation.
B12 and Folate
Treatment for megaloblastic anemia
Pernicious anemia is an example
Megaloblastic because cells lack the nutrients that allow them to divide. They just get larger.
Deferoxamine mesylate
Chelation agent used to treat iron toxicity
Folate
Required for DNA synthesis
Deficiency is a cause if megaloblastic anemia
Metabolized to THF in order to be used
Less than 5ng/ml is deficiency
Increased requirement in pregnancy
Make sure that your diagnosis is right, because if the patient’s anemia is due to B12 deficiency and you treat with only folate, you’ll have CNS damage.
Vitamin b12
Cofactors for enzyme… Look them up.
Microgram requirement as opposed to nanogram requirement for folate
Erythropoietin
Increases the production of erythrocytes Released by kidney cells These cells respond to oxygen levels. Cloned product from recombinant DNA Used to treat anemia associated with AIDS and with chemotherapy May worsen hypertension May increase chance of clotting.
Filgrastim G-CSF
Stimulates neutrophil production
Sargramostim GM-CSF
Stimulates production of granulocytes and macrophages
Sodium Bicarbonate
Classic antacid.
Neutralizes HCl, producing NaCl, H2O, and CO2.
CO2 can cause distention
Works fast, but doesnt last long.
Can cause metabolic alkalosis.
Can cause problems associated with high Na intake.
Used in tx of heartburn and mild gastritis.
NOT useful for peptic ulcer disease.
Calcium Carbonate
Antacid.
Neutralizes HCl, producing CaCl2, H2O, and CO2.
Can cause metabolic alkalosis, especially in patients with high Ca intake or poor renal fxn.
Can cause rebound acid excretion.
NOT good for long term management of peptic ulcers.
Can form complexes with some other drugs, decreasing their bioavailability.
Magnesium Hydroxide
Antacid.
Neutralizes HCl, producing MgCl2 and H2O. (No CO2 production).
Not well absorbed so it doesnt cause metabolic alkalosis like the other antacids.
Can have diarrhetic effect.
Poor renal function can cause Mg build-up (hypermagnesemia).
Like Calcium Carbonate, can for complexes with many drugs, decreasing their bioavailability.
Maalox
Aluminum hydroxide plus Magnesium hydroxide.
Combination antacid.
They are combined to minimize the side effects of each individual agent.
4 H2 Antagonists
Famotidine
Ranitidine
Cimetidine
Nizatidine
Used in the tx of peptic ulcer disease (acute and preventative treatment)
Also used to treat Zollinger Ellison and GERD.
4 Proton Pump Inhibitors
Pantoprazole
Omeprazole
Lanzoprazole
Esomeprazole
Pantoprazole, Omeprazole, Lanzoprazole, Esomeprazole.
Proton Pump Inhibitors.
Reduce most types of acid secretion.
Some activity against H. pylori.
Taken as prodrugs, metabolized to agents the covalently interact with proton pumps.
Need to be taken on empty stomach.
Take 3-4 days to have effect.
Very effective tx for ZE, peptic ulcers, GERD.
Inhibit hepatic drug metabolizing enzymes (can have drug interactions)
May allow overgrowth of upper GI tract bacteria.
Maybe increases risk of bone fractures in females???
Sucralfate
Polymerizes in stomach to form viscous coating that covers ulcer and forms protective barrier.
Needs acidic stomach to work (don’t take with antacids)
Side effect is constipation.
Can form complexes with other drugs.
Can cause Al buildup in patients with impaired renal fxn.
Misoprostol
PGE 1 Analogue
Increases mucus production and decreases acid secretion.
Used to prevent NSAID induced GI ulcers.
Can induce uterine contractions because it’s a prostaglandin. DONE USE IN PREGNANT FEMALES or those who may become pregnant.
Bismuth compounds
Coat the stomach and inhibit actions of pepsin.
Protects against ulceration.
Treatment of H. pylori infection
Usually either a PPI or a bismuth compound in addition to 1-2 antibiotics (Clarithromycin, Amoxicillin, metronizadole, tetracycline).
What is the difference between a laxative, cathartic, and a purgative?
Laxatives are the mildest, form soft stool over a period of hours/days.
Cathartics are more intense, produce a prompt, fluid evacuation.
Purgatives are super intense, cause pain/cramping, clean you out goooood.
Dietary Fiber
Bulk forming laxative.
Mostly cellulose, indigestible carbs. Helps you poop, decreases risk of colon cancer.
Methylcellulose
Bulk forming laxative.
Synthetic cellulose, fiber.
Psyllium
Bulk forming laxative.
Fiber from Plantago seeds.
Polycarbophil
Bulk forming laxative.
Polyacrylic resin.
Phenolphthalein
Laxative
Inhibits absorption of water in the bowel.
Can have systemic effects.
Turns urine red if it’s basic.
Carcinogenic? Maybe, that’s why we don’t use it.
Bisacodyl
Laxative that inhibits water absorption in the bowels.
Senna
Laxative with effects similar to bisacodyl.
Plant extract that contains anthraquinone compounds in glycoside linkages.
Castor Oil
Laxative.
Hydrolyzed in small intestine to ricinoleic acid, the active agent.
Acts in small intestine to decrease water absorption and stimulate peristalsis.
Can produce intense effects, which is why it’s no longer recommended.
Magnesium hydroxide (laxative)
Osmotic laxative.
Poorly absorbed salt that exerts an osmotic effect, preventing water absorption.
Causes fluid evacuation within 1-6 hours.
Polyethylene glycol
Osmotic laxative.
Used in combo with other laxatives to prepare bowel for surgical/endoscopic procedures.
Mineral Oil
Lubricating agent to help you poop.
Petroleum product.
Aspiration can cause lipid pneumonitis.
Can decrease absorption of fat soluble vitamins (ADEK).
Can leak from your anus and stain furniture…
Docusate sodium
Surface active agent (fecal softener)
Detergent breaks up fecal mass.
May increase solubility/absorption of other drugs.
Lubiprostone
Treats idiopathic constipation and constipation in IBS.
Activates chloride channels in the intestines, increasing fluid secretion.
Typical GI side effects.
Safe for pregnancy? Who knows.
Linaclotide
Treats idiopathic constipation and constipation in IBS.
Activates gunnel cyclase, increasing cGMP, which enhances fluid secretion in the GI tract.
Side effects include diarrhea, cramping, and dehydration.
Don’t give it to kids, they’re at higher risk of dehydration.
Methylnaltrexone and Alvimopan
Quaternary opioid antagonists used to treat opioid induced constipation.
Methylnaltrexone is given parenterally, which Alvimopan can be given orally.
Only appropriate for serious constipation caused by high dose opioid tx.
Also used for paralytic ileus.
Contraindications for laxative use
Nausea/vomiting Abdominal cramps Undiagnosed abdominal pain Appendicitis Intestinal Obstruction
Loperamide
Anti-diarrhetic
Opioid analog that decreases peristalsis without having CNS effects.
Now available OTC.
If P-gp is inhibited, loperamide can better cross the BBB and may have CNS effects.
Atropine, propantheline, dicyclomine
Anticholinergics used to treat irritable bowel syndrome.
Colloidal bismuth compoinds
General anti diarrhetic. Absorbs excess water. May inhibit some bacterial toxins. Darkens stool. Dont give to kids because you may cause Reye's.
Sulfazaline
Converted in bowel to sulfapyridine and aminosalicyclic acid.
Aminosalicyclic acid has an anti-inflammatory effect (effective in UC) and sulfapyridine has antimicrobial activity.
Don’t give it to people allergic to sulfa…
Infliximab
mab that binds and inactivated TNFalpha and suppresses immune fxn.
Tx for Crohn’s disease.
Given via IV.
Works for some, not for others.
Can cause hypersensitivity reactions and make patients more prone to infections.
Bethanechol
Cholinergic agonist that increases GI tone and motility.
Erythromycin
Antimicrobial agent that also stimulates motion and promotes gastric emptying.
Sometimes used to treat gastroparesis.
Simethicone
Antiflatulant
Surface active agent that prevents formation of large gas bubbles.
Does it work? ¯_(ツ)_/¯
Lactase
Digests lactose in people who can’t.
Keeps you from farting.
Alpha-D-galactosidase
Digests galactose in people who can’t.
Keeps you from farting.
10 Mu Agonists
Morphine Codeine Fentanyl Heroin Hydrocodone Hydromorphone Meperidine Methadone Oxycodone Oxymorphone
5 Partial/Mixed Opioid Agonists
Pentazocine Buprenorphine Butorphanol Tramadol Tapentadol
5 Opioid Antagonists
Naloxone Naltrexone Methylnaltrexone Alvimopan Naloxegol
Difference between an Opiate, an Opioid, and a narcotic.
Opiate means derived from opium.
Opioid means having properties similar to drugs derived from opium.
Narcotic means sleep inducing, but more commonly is used to mean “opioid.”
What receptor effects do morphine, hydromorphone, pentazocine, nalbuphine, buprenorphine, and naloxone have?
Morphine is mostly Mu, but also agonist at kappa and delta.
Hydromorphone is the same as morphine.
Pentazocine is a kappa agonist.
Nalbuphine is a mu antagonist and a kappa agonist.
Buprenorphine is the opposite of nalbuphine (mu agonist and kappa antagonist).
Naloxone is an antagonist at mu, kappa, and delta.
