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Beta blockers:
B1 selective vs. B1-B2 non-selective
A through N: B1 selective: Acebutalol, Atenolol, Esmolol, Metoprolol.
O through Z: B1, B2 non-selective: Pindolol, Propanalol, Timolol.
Narcotics: side effects "SCRAM if you see a drug dealer": Synergistic CNS depression with other
drugs
Constipation
Respiratory depression
Addiction
Miosis
Sex hormone drugs: male "Feminine Males Need Testosterone":
Fluoxymesterone
Methyltestosterone
Nandrolone
Testosterone
Disulfiram-like reaction inducing drugs "PM PMT" as in Pre Medical Test in the PM:
Procarbazine
Metronidazole
Cefo (Perazone, Mandole, Tetan).
Diuretics:
thiazides: indications "CHIC to use thiazides":
CHF
Hypertension
Insipidous
Calcium calculi
Tetracycline: teratogenicity
TEtracycline is a TEratogen that causes staining of TEeth in the newborn.
Patent ductus arteriosus: treatment
"Come In and Close the door": INdomethacin is used to Close PDA.
Reserpine action:
Reserpine depletes the Reserves of catecholamines [and serotonin].
Succinylcholine:
action, use Succinylcholine gets Stuck to Ach receptor, then Sucks ions in through open pore.
You Suck stuff in through a mouth-tube, and drug is used for intubation.
Beta-blockers: side effects "BBC Loses Viewers In Rochedale": Bradycardia
Bronchoconstriction
Claudication
Lipids
Vivid dreams & nightmares
-ve Inotropic action
Reduced sensitivity to hypoglycaemia
Cisplatin: major side effect, action "Ci-Splat-In":
Major side effect: Splat (vomiting sound)--vomiting so severe that anti-nausea drug needed. Action:
Goes Into the DNA strand.
Vir-named drugs: use"-vir at start, middle or end means for virus": · Drugs:
Abacavir,
Acyclovir,
Amprenavir,
Cidofovir,
Denavir,
Efavirenz,
Indavir,
Invirase,
Famvir,
Ganciclovir,
Norvir,
Oseltamivir,
Penciclovir,
Ritonavir,
Saquinavir,
Valacyclovir,
Viracept,
Viramune,
Zanamivir,
Zovirax.
Prazocin: usage
Prazocin sounds like an acronym of "praszz zour urine".
Therefore Prazocin used for urinary retention in BPH.
Bleomycin: action
"Bleo-Mycin Blows My DNA to bits": Bleomycin works by fragmenting DNA (blowing it to
bits). My DNA signals that its used for cancer (targeting self cells).
Enoxaprin (prototype low molecular weight heparin): action, monitoring EnoXaprin only acts
on factor Xa. Monitor Xa concentration, rather than APTT.
Propranolol and related '-olol' drugs: usage"olol" is just two backwards lower case b's.
Backward b's stand for "beta blocker". · Beta blockers include acebutolol, betaxolol, bisoprolol,
oxprenolol, propranolol.
Benzodiazapines: ones not metabolized by the liver (safe to use in liver failure)
LOT:Lorazepam Oxazepam Temazepam
Benzodiazepines: actions
"Ben SCAMs Pam into seduction not by brain but by muscle":
Sedation
anti-Convulsant
anti-Anxiety
Muscle relaxant
Not by brain: No antipsychotic activity.
Beta-blockers:
nonselective beta-blockers"Tim Pinches His Nasal Problem"
(because he has a runny nose...):
Timolol
Pindolol
Hismolol
Naldolol
Propranolol
Methyldopa:
side effects METHYLDOPA:
Mental retardation
Electrolyte imbalance
Tolerance
Headache/ Hepatotoxicity psYcological upset
Lactation in female
Dry mouth
Oedema
Parkinsonism
Anaemia (haemolytic)
B. Opiate Agonists (Morphine, Meperidine, Codeine, Methadone, Heroin, Fentanyl) • Act at mu, kappa,
delta receptors in CNS • Analgesia; Antitussive (Codeine); opiate addiction (Methadone); antidiarrheal
(loperamide) • CNS depression; nausea; respiratory depression; constipation; urinary retention;
dependence
Opiate Mixed Agonists-Antagonists (Pentazocine) • Same as agonists but will cause withdrawal in those
dependent on agonists
Opiate Antagonists (Naloxone, Naltrexone) • Block opiate receptors • Narcotic overdose (no effect if used
alone)
Erythropoietin • Increases RBC production in marrow • Anemia associated with renal failure
RU486 (Mifepristone) • Progestin antagonist • Early-term abortion • Uterine bleeding, possible incomplete
abortion
G. Flutamide • Blocks inhibitory effects of testosterone on GnRH release • Combo with leuprolide
I. Metformin • Decreases gluconeogenesis; improves lipid profile (HDL rises, LDL falls) • NIDDM – lower
risk of hypoglycemia • GI side effects; lactic acidosis (rare); long-term interference w B12 absorption
J. Stool Softeners (psyllium, methylcellulose) • Absorbs water and softens stool bulk peristalsis •
Constipation Mechanism, clinical use, and toxicity of dermatologic agents: CORTICOSTEROIDS:
Synthesized in the zona fascilculata of the adrenal cortex. Cortisol and Cortisone produced. 1)
Glucocorticoids are catabolic. They influence carbohydrate and fat metabolism to insure adequate
delivery of glucose to brain and tissues. 2) Decrease intestinal uptake of calcium; increase renal excretion
of calcium (contribute to osteoporosis). 3) Supress the inflammatory response – Decrease edema, fibrin
deposition, capillary dilatation, leukocyte migration and phagocytic activity. Inhibit prostaglandin and
leukotriene production by inhibiting phospholipase A2. 4) Include: Cortisone (short acting), Prednisone
(intermediate acting), Prednisolone (similar to prednisone but no hepatic metabolism for activity),
Methylprednisolone (similar to prednisolone but better anti-inflamatory and less mineralocorticoid
effects), Triamcinolone (5x more potent than cortisol), Dexamethasone (long acting) & Beclomethasone
(long acting available as aerosol). 5) Toxicity: a) Skin: hirsutism, skin thinning, poor wound healing,
striae, acne and purpura. b) Other: hyperglycemia, hypertension, cataracts, glaucoma, peptic ulcer
disease, osteoporosis, and increased susceptibility to infection.
RETINOIDS: 1) Used to treat the following dermatologic diseases: Acne, psoriasis, icthyosis and has a
potential benefit in early skin cancers (actinic keratosis) 2) Toxicity: in skin it can cause desquamation,
dry skin and pruritus, erythema.
ANTIFUNGALS: 1) Polyene antibiotics are fungicidal against both filamentous and yeastlike fungi including
Histoplasma, Blastomyces, Coccidioides, Cryptococcus, Candida, Aspergillus and Sporothrix. Polyenes
interact with sterols in the cytoplasmic membrane of fungi leading to rapid leakage of small molecules
and death. Sensitive fungi have ergosterol in their membranes. a) Amphotercin B: Broad spectrum to
treat systemic fungal infections. Side effects: Fever, chills, impaired renal function, anemia,
thrombocytopenia. b) Nystatin (Mycostatin): Similar to A but used primarily in topical preparations. Use in
Candida infections and prophylaxis. 2) Imidazoles: Block the synthesis of fungal cell membrane
ergosterols. a) Miconazole & Clomitrazole: Miconazole is the only imidazole that can be administered IV;
clotrimazole is only used topically. i) Intravenous miconazole is rarely used due to toxicity. Treats
ringworm, vulvovaginal candidiasis b) Ketoconazole: Oral administration only. Causes gynecomastia. 3)
Miscellaneous: a) Flucytosine: Administer with amphotercin B in the treatment of cryptococcal meningitis
and other systemic infections (synergistic). b) Griseofulvin: Binds to keratin, treat Tineas (capitis, corporis
etc),
Other new pharmacologic agents: 1) Erythopoietin (EPO): RBC growth factor. Produced in kindneys.
Recombinant form available (epoietin alpha). a) Use for tx of Anemia 2nd to renal failure or zidovudine
(AZT) use HIV patients. b) Use for tx of Anemia 2nd to chemo, or to stimulate rbc production prior to
surgery or to facilitate autologous donation. c) Side effects: Clotting of dialysis tubing and hypertension.
2) RU486 (Mifrepristone): Abortificen. Blocks progesterone receptors and thereby progesterone support
of pregnancy. 80% effective, 95% if used with prostaglandins. a) Complications include incomplete
abortion (2%), ongoing pregnancy (1%), hemorrhage during D&C (<1%). Know About......
1) Complications of empiric antibiotic use: a) Resistance: Must take into account susceptibility patterns of
local settings. Must distinguish between community vs. nosocomial infection, and must take into account
the patient’s immune status. b) Fungal Infections: Due to destruction of normal flora. (candidiasis). c)
Other complications: C. Diff Pseudomembranous colitis. Gentamicin ototoxicity (must monitor levels),
Sulfonamides and Penicillin allergic reactions. 2) Secondary effects of other drugs: a)
Heparinosteoporosis with chronic use. Thombocytopenia – usually transient and mild. b)
ThiazidesHyperlipidemia, hypokalemia. 3) Drugs that block/increase hepatic drug metabolism: a)
Cimetidine: Histamine analog that cab reduce hepatic blood flow and slow clearance of other drugs and
also reduces activity of cytochrome p-450 b) Ethanol: Chronic use induces hepatic microsomal enzymes
and may enhance metabolism of other drugs. c) Phenobarbital: Increased phenobarbital levels in patients
that have ethanol, chloramphenicol or valproic acid on board, since it has microsomal enzyme
metabolism. d) Phenytoin (Dilantin): same as Phenobarb and ETOHMetabolized by microsomal
enzymes. e) Rifampin: Causes jaundice and hepatotoxicity, also interacts with C p-450 system. 4)
Fundamental Pharmacodinamics: a) Partial agonists/agonist: Drugs that bind to receptors and stimulate
them. b) Antagonists: are drugs that bind to receptors and decrease or block the effect of an agonist.
They do not stimulate the receptors. i) Competitive antagonist: Reversibly binds to the receptor and
prevents binding of the agonist. ii) Non competitive antagonist: Usually binds to the receptor irreversibly
and prevents any agonist action. c) Efficacy: Maximal effect produced by a drug. d) Potency: Activity of a
drug compared to a reference standard; depends on the drug’s ability to reach the receptors and its
affinity to the receptor. 5) Drug efficacy and potency as demonstrated on dose-response curves: a) ED50
(effect dose)- Dose which produces half-maximal response (ie., observed effect seen in 50% of patients);
used as a measure of potency (the lower the ED50, the more potent the drug). b) TD50 (toxic dose)-
Minimum dose which produces a specific toxic effect in 50% of individual (or animals). c) LD50 (lethal
dose)- Minimum dose which kills 50% of animals. d) Therapeutic index- Ratio of dose required to
produce a toxic effect to the dose needed for a therapeutic effect. Used as an indication of drug safety.
Expressed as :
TI= TD50 or TI= LD50 You want drugs with a high therapeutic index (low ED 50 ED50 side effects at
usual doses).
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