PHARM elective Flashcards
USES: Oncology; IV and Topical.
MOA: Included in antimetabolite and pyrimidine analog families of medications believed to involve blocking the action of thymidylate synthase and thus stopping the production of DNA.
AE: Common side effects include anorexia, mucositis, low blood cell counts, hair loss, cardiotoxicity, neurotoxicity and dermatitis.
5-fluorouracil
USES: Anti-Parkinson; Anti-viral, MS (anti-fatigue) – NOT first line for any indication.
MOA: Parkinson’s: Weak antagonist of the NMDA-type glutamate receptor, increases dopamine release, and blocks dopamine reuptake. Antiviral and antiparkinsonian effects are unrelated. Antiviral activity involves interference with the viral protein, M2, a proton channel then with entry of the virus into cells blocks replication.
AE: Central nervous system side effects nervousness, anxiety, agitation, insomnia, difficulty in concentrating, and exacerbations of pre-existing seizure disorders and psychiatric symptoms in patients with schizophrenia or Parkinson’s disease (think dopamine and autonomic effects). Rare cases of severe skin rashes, such as Stevens-Johnson syndrome and of suicidal ideation have also been reported in patients treated with …. Livedo reticularis is a possible side effect of … use for Parkinson’s disease.
Amantadine
USES: Treats parasitic worm infestations. Primarily; giardiasis, trichuriasis, filariasis, neurocysticercosis, hydatid disease, pinworm disease, and ascariasis, among others. PO drug.
MOA: Creates degeneration in the intestinal cells of the worm. The loss of the cytoplasmic microtubules leads to impaired uptake of glucose by the larval and adult stages of the susceptible parasites and are immobilized and eventually die.
AE: Nausea, abdominal pain, and headaches. Bone marrow suppression (transient, usually resolves with d/c). Potential hepatotoxicity. Pregnancy category C in the United States.
DRUG-DRUG: Antiepileptics: carbamazepine, phenytoin, and phenobarbital lower the plasmatic concentration and the half life of …. H2 Blocker: Cimetidine heightens serum … / increases the half-life of …. May boost the potency of …..
Albendazole
USES: Babies with congenital heart defects given IV to open the ductus arteriosus until surgery can be carried out. Penile injection or placement in the urethra for erectile dysfunction.
MOA: Prostaglandin E1 is a vasodilator; opening blood vessels by relaxing smooth muscle.
AE: Common side effects in babies include bradypnia, fever, and hypotention. In erectile dysfunction side effects may include penile pain, bleeding at the site of injection, and priapism.
Alprostadil (PGE-1)
USES: Norepinephrine reuptake inhibitor approved for the treatment of attention deficit hyperactivity disorder
MOA: NE reuptake inhibition.
AE: GI (Nausea, Anorexia), Seizure, Cardiovasuclar, Erectile dysfunction, Fatigue, Headache, Cough.
DRUG-DRUG: Substrate for CYP2D6 so concurrent treatment with CYP2D6 inhibitors such as bupropion (Wellbutrin) or fluoxetine (Prozac) is not recommended. Antihypertensive and pressor (dopamine etc.) agents, due to the additive effect of indirect sympathomimetics such as atomoxetine. Norepinephrine- acting agents such as α1 adrenoceptor agonists or norepinephrine reuptake inhibitors due to the potential for additive or synergistic pharmacologic effects.
Atomoxetine
USES: Antitussive
MOA: Non-narcotic - local anesthetic, decreasing the sensitivity of stretch receptors in the lower airway and lung reducing the cough reflex upon inspiration. Chemically related to other ester anesthetics such as procaine and tetracaine.
AE: Common - drowsiness, dizziness, and dysphagia. Overdose may manifest as central nervous system side effects, such as mental confusion and hallucination, restlessness and tremors, and in extreme cases convulsions and death.
DRUG-DRUG: CI in PABA allergy / Ester anesthetic allergy. Theoretical OD potential with other anesthetics.
Benzonatate (Tessalon)
USES: Parkinson’s, Dystonia, Reduce antipsychotic AE’s.
MOA: Anticholinergic. Centrally acting anticholinergic/antihistamine agent. Selective M1 muscarinic acetylcholine receptor antagonist. Partially blocks cholinergic activity in the basal ganglia and has also been shown to increase the availability of dopamine (Blocks DA reuptake).
AE: [THINK BELLADONNA] Dry mouth, Blurred vision, Cognitive changes, Constipation, Urinary retention, Tachycardia, Anorexia and in overdose: Psychosis.
Benztropine (cogentin)
USES: Xerostomia. Orally or subcutaneously to treat urinary retention resulting from general anesthetic, diabetic neuropathy of the bladder, or a side effect of antidepressants. Also to treat gastrointestinal lack of atony. Atropine reversal: Atropine is given preoperatively to prevent voiding of the bowel/bladder during surgery, … is then given postoperatively to revert this action.
MOA: Parasympathomimetic (muscarinic receptors but no effect on nicotinic receptors).
AE: … should be used to treat these disorders only after mechanical obstruction is ruled out as a possible cause.
DRUG-DRUG: Parasympathomimetic drug synergy (Pilocarpine) – possible OD.
Bethanechol
USES: Oral. Primarily used together with a gonadotropin-releasing hormone (GnRH) analogue or surgical removal of the testicles to treat metastatic prostate cancer. Also: excessive hair growth in women, a component of hormone therapy for transgender women, prevention of priapism, and to treat early puberty in males.
MOA: Antiandrogen non-steroidal antiandrogen (NSAA), blocks the androgen receptor.
AE: In severe hepatic impairment t ½ is increased and the drug is contraindicated. Pregnancy Cat-X. Liver function test elevation is common. Rare AE in women however either gender may include diarrhea, constipation, abdominal pain, nausea and dermatologic effects. MALES - THINK: androgen deprivation. Breast pain/tenderness and gynecomastia. Physical feminization, hot flashes, sexual dysfunction (including loss of libido and erectile dysfunction), depression, fatigue, weakness, anemia, and decreased semen/ejaculate volume.
DRUG-DRUG: Exclusively metabolized by CYP3A4 (which is the most common ‘CYP’ drugs are processed through) but no evidence of clinically significant drug interactions when used at a standard dose and is co-administered with drugs that inhibit or induce cytochrome P450 enzyme activity.
Bicalutamide
USES: Muscle spasticity, Other muscle disorders, Migraine, Cosmetic
MOA: prevents the release of the neurotransmitter acetylcholine from axon endings at the neuromuscular junction and thus causes flaccid paralysis.
AE: Most commonly, … toxin can be injected into the wrong muscle group or spread from the injection site, causing paralysis of unintended muscles. Severe AE’s from therapeutic use can include arrhythmia, heart attack, and in some cases seizures, respiratory arrest, and death
Botulinum toxin
USES: Crohn’s and Colitis
MOA: Glucocorticoid AE:
Steroid AE’s (see main review)
DRUG-DRUG: Grapefruit juice may double bioavailability of oral …. Echinacea diminishes bioavailability.
Budesonide
USES: used to treat opioid addiction, moderate acute pain and moderate chronic pain. The combination …/naloxone [Suboxone] is also used for opioid addiction.
MOA: Opioid; semisynthetic derivative of thebaine and a mixed partial agonist opioid receptor modulator
AE: Similar to those of other opioids: nausea and vomiting, drowsiness, dizziness, headache, memory loss, cognitive and neural inhibition, perspiration, itchiness, dry mouth, miosis, orthostatic hypotension, male ejaculatory difficulty, decreased libido, and urinary retention. *Constipation and CNS effects are seen less frequently than with morphine.
DRUG-DRUG: Opiates – Additive effect.
Buprenorphine (Subutex)
USES: DM-2
MOA: Gliflozin class or subtype 2 sodium-glucose transport (SGLT-2) inhibitors class. Increases urinary excretion of glucose. (See main review notes on diabetic medications).
AE: increased incidence of urinary tract infections, fungal infections of the genital area, thirst, elevations in LDL cholesterol, increased urination and episodes of low blood pressure. Concerns that it may also increase the risk of diabetic ketoacidosis. Multiple references to potential cardiovascular problems.
DRUG-DRUG: increase the risk of dehydration in combination with diuretic drugs.
Canagliflozin
USES: Oncology
MOA: Partial oxidant as well as binding to and blocking the duplication of DNA
AE: side effects include bone marrow suppression, hearing damage, kidney damage, nausea and vomiting. Other include neuropathy, ataxia, allergic reactions, electrolyte problems, and cardiac
damage. Use in pregnancy is known to harm the fetus.
Cisplatin
USES: Various skin conditions including eczema and psoriasis and for contact dermatitis (TOPICAL use)
MOA: Corticosteroid of the glucocorticoid class
AE: See main clinical review. DRUG-DRUG: See main clinical review.
Clobetasol propionate
USES: Infertility in anovulation and PCOS. It is taken PO - QD. Also male hypogonadism as an alternative to testosterone replacement therapy.
MOA: Non-steroidal drug; inhibits estrogen receptors in the hypothalamus, inhibiting negative feedback of estrogen on gonadotropin release, leading to up-regulation of the hypothalamic–pituitary–gonadal axis, causing the release of gonadotrophin by the hypothalamus. Is a selective estrogen receptor modulator (SERM) medication.
AE: Common - pelvic pain and hot flushes. Other - changes in vision, vomiting, insomnia, ovarian cancer, and seizures. Not recommended in liver disease or pregnancy. Use results in a greater chance of twins.
Clomiphene
USES: Elevated cholesterol, GI binding agent.
MOA: Bile acid sequestrant used PO.
AE & DRUG-DRUG: See main review “Cholestyramine”.
Colesevelam
USES: Oncology and Nephrotic Syndrome (as an immunosuppressant).
MOA: Alkylating agent (nitrogen mustard family). Interferes with the duplication of DNA and the creation of RNA.
AE: Nausea and vomiting, bone marrow suppression, GI Pain / Diarrhea, hemorrhagic cystitis, darkening of the skin/nails, alopecia and lethargy. Others may include easy bruising/bleeding, arthralgias, mucositis, slow-healing wounds, oliguria and fatigue. Rarely - Pulmonary damage.
Cyclophosphamide
USES: Anticoagulant
MOA: Direct thrombin inhibitor.
AE: Bleeding - In case of major bleeding: antidote is idarucizumab. GI upset due to increased acidification of the stomach.
DRUG-DRUG: In patients on p-glycoprotein pump inhibitors such as quinidine, verapamil, and amiodarone a potential increase in plasma levels of … exists.
Dabigatran
USES: Treatment of osteoporosis, treatment-induced bone loss, metastases (bone), and giant cell tumors (bone).
MOA: Human monoclonal antibody “MAB” a RANKL (a part of T-Helper cells) inhibitor which works by preventing the development of osteoclasts. ** Sufficient calcium and vitamin D levels must be reached before starting on ….
AE: Common side effects are joint and muscle pain in the arms or legs; contraindicated in hypocalcemia. Increased infection risk, increased eczema, osteonecrosis of the jaw and atypical femur fractures
DRUG-DRUG: Unknown
Denosumab
USES: Joint pain.
MOA: NSAID (Is a minimally systemic prescription topical lotion formulation of 1.5% diclofenac sodium).
AE: Topical are rare. Dermatitis may occur.
Diclofenac gel
USES: Hypertension therapy and urinary retention associated with benign prostatic hyperplasia. Off label for PTSD nightmares.
MOA: An α1-selective alpha blocker.
AE: Hypotention.
DRUG-DRUG: Caution with other hypertensive medications.
Doxazosin
USES: Birth control, Acne, PMDD.
MOA: Inhibition of ovulation.
AE: Reports of up to sevenfold risk of developing thromboembolism. FDA packaging update: “stop pre and post-surgery”.
DRUG-DRUG: In mild or moderate renal insufficiency, or in combination with chronic daily use of other potassium-sparing medications (ACE inhibitors, angiotensin II receptor antagonists, potassium-sparing diuretics, heparin, aldosterone antagonists, or NSAIDs): Potassium level should be checked after two weeks of use.
Drospirenone/ethinyl estradiol (yasmin)
USES: Emboli (PE, DVT…), Acute Coronary Artery Syndrome
MOA: A low molecular weight heparin
AE: Bleeding, LFT elevation, TTP, anemia, dyspnea. BLACK BOX WARNING FOR PEOPLE HAVING SPINAL CATHETERS PLACED (to avoid the drug).
DRUG-DRUG: Many other anticoagulants enhance effect especially NSAIDS. Antidote = Protamine sulfate or heparin which is the best antidote.
Enoxaparin
USES: Primary US approval for rheumatoid arthritis, juvenile rheumatoid arthritis, psoriatic arthritis, plaque psoriasis and ankylosing spondylitis.
MOA: TNFa Blocker
AE: BLACK BOX warning: Serious infections and sepsis, including fatalities, have been reported with the use of … including reactivation of latent tuberculosis and hepatitis B infections. (See prior slides, increased incidence of cancer is reported.)
Etanercept
USES: Cholesterol lowering therapy. Second line therapy for those intolerant of statins or unable to achieve target LDL cholesterol levels
MOA: Blocks absorption of cholesterol from the small intestine and decreases the amount of cholesterol normally available to liver cells, leading them to absorb more from circulation (lowering levels of circulating cholesterol).
AE: Main contraindications: a previous allergic reaction (including rash, angioedema, and anaphylaxis) and severe liver disease. *Increased when taken with a statin.
DRUG-DRUG: May have significant interactions with cyclosporine and ‘fibrates’ other than fenofibrate.
Ezetimibe
USES: MS (immunomodulator)
MOA: A sphingosine-1-phosphate receptor modulator (sequesters lymphocytes in lymph nodes) decreasing autoimmune reaction.
AE: Common: URI, headache, and fatigue. Rare: skin cancer, potentially fatal infections, bradycardia, hemorrhaging focal encephalitis (Brain inflammation with bleeding). Fatal: Brain HHV infection, and a case of zoster. Also: progressive multifocal leukoencephalopathy and macular edema.
Fingolimod
USES: Class I-C antiarrhythmic agent indicated in: tachyarrhythmias, paroxysmal atrial fibrillation, paroxysmal supraventricular tachycardia, WPW and ventricular tachycardia.
MOA: Sodium channel blocker in the heart, slowing AP upstroke and prolongation of the cardiac AP.
AE: Cardiac and Pulmonary toxicity.
DRUG-DRUG: Alcohol: (decreased CV function). Amiodarone and Quinidine: inhibit CYP450 2D6 increase … levels. Cimetidine: increases … levels by 30% / half-life by 10%. Digoxin: increase digoxin levels. Paroxetine: increased effect of both drugs. Propafenone: increased effect of both drugs and increased risk of toxicity.
Flecainide
USES: Added to hydrocortisone in adrenal insufficiency. First line: Orthostatic intolerance and postural orthostatic tachycardia syndrome (POTS). Hypotension.
MOA: Mineralocorticoid with minor glucocorticoid effect.
AE: Common side effects: Hypertension, edema, heart failure, increased sodium / low blood potassium, low immune system, cataracts, muscle weakness, and mood changes.
Fludrocortisone
USES: Allergic rhinitis
MOA: Corticosteroid
AE: See main clinical review.
Fluocinonide-nasal spray
USES: Hyperlipidemia (Type III) and Hypertriglyceridemia (Type IV) – See Fredrickson’s Genotypes in the main review.
MOA: A ‘fibrate’ class drug: Exact MOA is unknown, theories include; inhibit lipolysis and decrease subsequent hepatic fatty acid uptake & inhibit hepatic secretion of VLDL potentially decrease serum VLDL levels; increases HDL-cholesterol; MOA of HDL elevation is unknown.
AE: GI distress, Musculoskeletal pain, Increased gallstone formation, Hypokalemia and Increased risk of cancer.
DRUG-DRUG: Anticoagulants: … potentiates the action of warfarin and indanedione anticoagulants. Statin drugs: Concomitant administration increases the risk of muscle cramping, myopathy, and rhabdomyolysis. Inhibits Cytochrome P450 system, reducing hepatic metabolism of many drugs, prolonging half-lives and duration of action.
Gemfibrozil
USES: SQ Injection in MS
MOA: Resembles myelin basic protein. Known to shift T cells from proinflammatory Th1 cells to regulatory Th2 cells that suppress the inflammatory response.
AE: Injection site reaction in approximately 30% of users, and aches, fever, chills (flu-like symptoms) in approximately 10% of users. Flushing, shortness in breath, anxiety and tachycardia soon after injection in up to 5% of patients typically blamed on IV injection which will subside within thirty minutes. Over time, a visible dent at the injection site (lipoatrophy) may develop as well at the injection site.
Glatiramer acetate
