Pulmonary infiltrations inducing drugs "Go BAN Me!

":

Gold

Bleomycin/ Busulphan/ BCNU

Amiodarone/ Acyclovir/ Azathioprine

Nitrofurantoin

Melphalan/ Methotrexate/ Methysergide

MPTP: mechanism, effect MPTP:

Mitochondrial Parkinson's-Type Poison.

· A mitochondrial poison that elicits a Parkinson's-type effect.

Antimuscarinics: members, action

"Inhibits Parasympathetic And Sweat":

Ipratropium Pirenzepine Atropine Scopolamine

· Muscarinic receptors at all parasympathetic endings sweat glands in sympathetic.

Teratogenic drugs: major non-antibiotics TAP CAP:

Thalidomide Androgens Progestins Corticosteroids Aspirin & indomethacin Phenytoin

Steroid side effects CUSHINGOID:

Cataracts

Ulcers

Skin: striae, thinning, bruising

Hypertension/ Hirsutism/ Hyperglycemia

Infections
Necrosis, avascular necrosis of the femoral head

Glycosuria

Osteoporosis, obesity

Immunosuppression

Diabetes

Beta blockers with CYP2D6 polymorphic metabolism

"I Met Tim Carver, the metabolic polymorph":

· The following beta blockers require dose adjustment due to CYP2D6 polymorphic metabolism:

Metoprolol Timolol Carvedilol (in patients with lower or higher than normal CYP2D6 activity)

Beta blockers with intrinsic sympathomimetic activity

Picture diabetic and asthmatic kids riding away on a cart that rolls on pinwheels. Pindolol and Carteolol
have high and moderate ISA respectively, making them acceptable for use in some diabetics or
asthmatics despite the fact that they are non-seletive beta blockers.

Muscarinic effects SLUG BAM:

Salivation/ Secretions/ Sweating

Lacrimation

Urination

Gastrointestinal upset

Bradycardia/ Bronchoconstriction/ Bowel movement

Abdominal cramps/ Anorexia

Miosis
Sulfonamide: major side effects

· Sulfonamide side effects:

Steven-Johnson syndrome

Skin rash

Solubility low (causes crystalluria)

Serum albumin displaced (causes newborn kernicterus and potentiation of other serum albumin-binders
like warfarin)

Epilepsy types, drugs of choice:

"Military General Attacked Weary Fighters Pronouncing 'Veni Vedi Veci' After Crushing Enemies":

· Epilepsy types: Myoclonic Grand mal Atonic West syndrome Focal Petit mal (absence)

· Respective drugs: Valproate Valproate Valproate ACTH Carbamazepine Ethosuximide

Quinolones [and Fluoroquinolones]: mechanism

"Topple the Queen": Quinolone interferes with Topoisomerase II.

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.

Ribavirin: indications RIBAvirin:

RSV

Influenza B

Arenaviruses (Lassa, Bolivian, etc.)

Hypertension: treatment ABCD:

ACE inhibitors/ AngII antagonists (sometimes Alpha agonists also) Beta blockers

Calcium antagonists

Diuretics

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

Ca++ channel blockers: uses CA++ MASH:

Cerebral vasospasm/ CHF

Angina

Migranes

Atrial flutter, fibrillation

Supraventricular tachycardia

Hypertension

· Alternatively: "CHASM":

Cererbral vasospasm / CHF

Hypertension
Angina

Suprventricular tachyarrhythmia

Migranes

Disulfiram-like reaction inducing drugs "PM PMT" as in Pre Medical Test in the PM:

Procarbazine

Metronidazole

Cefo (Perazone, Mandole, Tetan).

Delerium-causing drugs ACUTE CHANGE IN MS:

Antibiotics (biaxin, penicillin, ciprofloxacin)

Cardiac drugs (digoxin, lidocaine)

Urinary incontinence drugs (anticholinergics)

Theophylline

Ethanol

Corticosteroids

H2 blockers

Antiparkinsonian drugs

Narcotics (esp. mepridine)

Geriatric psychiatric drugs

ENT drugs

Insomnia drugs

NSAIDs (eg indomethacin, naproxin)

Muscle relaxants

Seizure medicines
Morphine: side-effects MORPHINE:

Myosis

Out of it (sedation)

Respiratory depression

Pneumonia (aspiration)

Hypotension

Infrequency (constipation, urinary retention)

Nausea

Emesis

Therapeutic dosage: toxicity values for most commonly monitored medications

"The magic 2s":

Digitalis (.5-1.5) Toxicity = 2.

Lithium (.6-1.2) Toxicity = 2.

Theophylline (10-20) Toxicity = 20.

Dilantin (10-20) Toxicity = 20.

APAP (1-30) Toxicity = 200.

Diuretics:

thiazides: indications "CHIC to use thiazides":

CHF

Hypertension

Insipidous

Calcium calculi
Migraine: prophylaxis drugs

"Very Volatile Pharmacotherapeutic Agents For Migraine Prophylaxis":

Verpamil

Valproic acid

Pizotifen

Amitriptyline

Flunarizine

Methysergide

Propranolol

Adrenoceptors: vasomotor function of alpha vs. beta

ABCD:

Alpha = Constrict.

Beta = Dilate.

Antiarrhythmics: classification

I to IV MBA College

· In order of class I to IV:

Membrane stabilizers (class I)

Beta blockers

Action potential widening agents

Calcium channel blockers

Opiods: mu receptor effects "MD CARES":

Miosis

Dependency

Constipation

Analgesics

Respiratory depression

Euphoria

Sedation

Cancer drugs: time of action between DNA->mRNA ABCDEF: Alkylating agents

Bleomycin

Cisplastin

Dactinomycin/ Doxorubicin

Etoposide

Flutamide and other steroids or their antagonists (eg tamoxifen, leuprolide)

Busulfan: features ABCDEF:

Alkylating agent

Bone marrow suppression s/e

CML indication

Dark skin (hyperpigmentation) s/e

Endrocrine insufficiency (adrenal) s/e

Fibrosis (pulmonary) s/e

Tricyclic antidepressants: members worth knowing

"I have to hide, the CIA is after me":

Clomipramine Imipramine Amitrptyline

· If want the next 3 worth knowing, the DNDis also after me:

Desipramine Norrtriptyline Doxepin

Torsades de Pointes: drugs causing APACHE:

Amiodarone Procainamide Arsenium Cisapride Haloperidol Eritromycin

Serotonin syndrome: components Causes HARM:

Hyperthermia Autonomic instability (delirium) Rigidity Myoclonus

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.

Physostigmine vs. neostigmine LMNOP:

Lipid soluble

Miotic

Natural

Orally absorbed well

Physostigmine

· Neostigmine, on the contrary, is:

Water soluble

Used in myesthenia gravis

Synthetic

Poor oral absorption

Beta 1 selective blockers

"BEAM ONE up, Scotty":

Beta 1 blockers:

Esmolol

Atenolol

Metropolol

Antirheumatic agents (disease modifying): members

CHAMP:

Cyclophosphamide

Hydroxycloroquine and choloroquinine

Auranofin and other gold compounds

Methotrexate

Penicillamine

Auranofin, aurothioglucose: category and indication

Aurum is latin for "gold" (gold's chemical symbol is Au).

Generic Aur- drugs (Auranofin, Aurothioglucose) are gold compounds.

· If didn't learn yet that gold's indication is rheumatoid arthritis, AUR- Acts Upon Rheumatoid.

Antiarrhythmics: class III members BIAS:

Bretylium

Ibutilide

Amiodarone

Sotalol

MAOIs: indications MAOI'S:

Melancholic [classic name for atypical depression]

Anxiety

Obesity disorders [anorexia, bulemia]

Imagined illnesses [hypochondria]

Social phobias

· Listed in decreasing order of importance.

· Note MAOI is inside MelAnchOlIc.

SIADH-inducing drugs ABCD:

Analgesics: opioids, NSAIDs

Barbiturates

Cyclophosphamide/ Chlorpromazine/ Carbamazepine

Diuretic (thiazide)

K+ increasing agents K-BANK:

K-sparing diuretic

Beta blocker

ACEI

NSAID
K supplement

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.

Phenobarbitone: side effects

Children are annoying (hyperkinesia, irritability, insomnia, aggression).

Adults are dosy (sedation, dizziness, drowsiness).

Prazocin: usage

Prazocin sounds like an acronym of "praszz zour urine".

Therefore Prazocin used for urinary retention in BPH.

Opioids: effects BAD AMERICANS:

Bradycardia & hypotension

Anorexia

Diminished pupilary size

Analgesics

Miosis

Euphoria

Respiratory depression

Increased smooth muscle activity (biliary tract constriction) Constipation

Ameliorate cough reflex

Nausea and vomiting

Sedation

TB: antibiotics used

STRIPE:

STreptomycin Rifampicin Isoniazid Pyrizinamide Ethambutol

Phenytoin: adverse effects PHENYTOIN:

P-450 interactions

Hirsutism

Enlarged gums

Nystagmus

Yellow-browning of skin

Teratogenicity

Osteomalacia

Interference with B12 metabolism (hence anemia)

Neuropathies: vertigo, ataxia, and headache

The Narcotic Antagonists are NAloxone and NAltrexone. · Important clinically to treat narcotic overdose.

Thrombolytic agents USA:

Urokinase Streptokinase Alteplase (tPA)

Routes of entry: most rapid ways meds/toxins enter body

"Stick it, Sniff it, Suck it, Soak it":

Stick = Injection

Sniff = inhalation

Suck = ingestion

Soak = absorption

Asthma drugs: inhibitor action

zAfirlukast: Antagonist of LT

zIlueton: Inhibitor of 5-LO

Direct sympathomimetic catecholamines DINED:

Dopamine

Isoproterenol

Norepinephrine

Epinephrine

Dobutamine
Anticholinergic side effects

"Know the ABCD'S of anticholinergic side effects":

Anorexia

Blurry vision

Constipation/ Confusion

Dry Mouth

Sedation/ Stasis of urine

Atropine use: tachycardia or bradycardia

"A goes with B": Atropine used clinically to treat Bradycardia.

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).

Aspirin: side effects ASPIRIN:

Asthma

Salicyalism

Peptic ulcer disease/ Phosphorylation-oxidation uncoupling/ PPH/ Platelet disaggregation/ Premature

closure of PDA

Intestinal blood loss

Reye's syndrome

Idiosyncracy

Noise (tinnitus)
Lupus: drugs inducing it HIP:

Hydralazine

INH

Procanimide

Vigabatrin: mechanism Vi-GABA-Tr-In:

Via GABA Transferase Inhibition

Morphine: effects at mu receptor PEAR:

Physical dependence

Euphoria

Analgesia

Respiratory depression

Enoxaprin (prototype low molecular weight heparin): action, monitoring EnoXaprin only acts on factor
Xa. Monitor Xa concentration, rather than APTT.

Beta-1 vs Beta-2 receptor location "You have 1 heart and 2 lungs":

Beta-1 are therefore primarily on heart. Beta-2 primarily on lungs.

SSRIs: side effects SSRI:

Serotonin syndrome

Stimulate CNS

Reproductive disfunctions in male

Insomnia
Ipratropium: action Atropine is buried in the middle:

iprAtropium, so it behaves like Atropine.

Warfarin: action, monitoring WePT:

Warfarin works on the extrinsic pathway and is monitored by PT.

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.

Depression: 5 drugs causing it PROMS:

Propranolol

Reserpine

Oral contraceptives

Methyldopa

Steroids

Lead poisoning: presentation ABCDEFG:

Anemia

Basophilic stripping

Colicky pain

Diarrhea

Encephalopathy

Foot drop

Gum (lead line)

Myasthenia gravis: edrophonium vs. pyridostigmine

eDrophonium is for Diagnosis.

pyRIDostigmine is to get RID of symptoms.

Morphine: effects MORPHINES:

Miosis

Orthostatic hypotension

Respiratory depression

Pain supression

Histamine release/ Hormonal alterations

Increased ICT

Nausea

Euphoria

Sedation

Inhalation anesthetics SHINE:

Sevoflurane

Halothane

Isoflurane

Nitrous oxide

Enflurane

· If want the defunct Methoxyflurane too, make it MoonSHINE.

Cholinergics (eg organophosphates): effects

If you know these, you will be "LESS DUMB":

Lacrimation

Excitation of nicotinic synapses

Salivation

Sweating

Diarrhea

Urination

Micturition

Bronchoconstriction

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.

Botulism toxin: action, related bungarotoxin

Action: "Botulism Bottles up the Ach so it can't be the released":

Related bungarotoxin: "Botulism is related to Beta Bungarotoxin (beta-, not alpha-bungarotoxin--alpha

has different mechanism).
Teratogenic drugs "W/ TERATOgenic":

Warfarin

Thalidomide

Epileptic drugs: phenytoin, valproate, carbamazepine

Retinoid

ACE inhibitor

Third element: lithium

OCP and other hormones (eg danazol)

Gynaecomastia-causing drugs DISCOS:

Digoxin

Isoniazid

Spironolactone

Cimetidine

Oestrogens

Stilboestrol

Benzodiazepenes: drugs which decrease their metabolism

"I'm Overly Calm":

Isoniazid

Oral contraceptive pills

Cimetidine

· These drugs increase calming effect of BZDs by retarding metabolism.

Anesthesia: 4 stages "Anesthesiologists Enjoy S & M":

Analgesia

Excitement

Surgical anesthesia

Medullary paralysis

4-Aminopyradine (4-AP) use"4-AP is For AP":

For AP (action potential) propagation in Multiple Sclerosis.

Osmotic diuretics: members GUM:

Glycerol

Urea

Mannitol

Sodium valproate: side effects VALPROATE:

Vomiting

Alopecia

Liver toxicity

Pancreatitis/ Pancytopenia

Retention of fats (weight gain)

Oedema (peripheral oedema)

Appetite increase

Tremor

Enzyme inducer (liver)

Nitrofurantoin: major side effects NitroFurAntoin:

Neuropathy (peripheral neuropathy)

Fibrosis (pulmonary fibrosis)

Anemia (hemolytic anemia)

Zafirlukast, Montelukast, Cinalukast:

mechanism, usage"Zafir-luk-ast, Monte-luk-ast, Cina-luk-ast": · Anti-Lukotrienes for Asthma.

· Dazzle your oral examiner: Zafirlukast antagonizes leukotriene-4.

Zero order kinetics drugs (most common ones) "PEAZ (sounds like pees) out a constant amount":

Phenytoin

Ethanol

Aspirin

Zero order

· Someone that pees out a constant amount describes zero order kinetics (always the same amount out)

Hepatic necrosis: drugs causing focal to massive necrosis

"Very Angry Hepatocytes":

Valproic acid

Acetaminophen

Halothane

Steroids: side effects BECLOMETHASONE:

Buffalo hump

Easy bruising

Cataracts

Larger appetite

Obesity
Moonface

Euphoria

Thin arms & legs

Hypertension/ Hyperglycaemia

Avascular necrosis of femoral head

Skin thinning

Osteoporosis

Negative nitrogen balance

Emotional liability

Amiodarone: action, side effects 6 P's:

Prolongs action potential duration

Photosensitivity

Pigmentation of skin

Peripheral neuropathy

Pulmonary alveolitis and fibrosis

Peripheral conversion of T4 to T3 is inhibited -> hypothyroidism

Monoamine oxidase inhibitors:

Members "PIT of despair":

Phenelzine

Isocarboxazid

Tranylcypromine ·

A pit of despair, since MAOs treat depression

Warfarin: metabolism SLOW:

· Has a slow onset of action.

· A quicK Vitamin K antagonist, though.

Small lipid-soluble molecule

Liver: site of action

Oral route of administration.

Warfarin

Propythiouracil (PTU):

Mechanism It inhibits PTU:

Peroxidase/ Peripheral deiodination

Tyrosine iodination Union (coupling)

Antibiotics contraindicated during pregnancy MCAT:

Metronidazole

Chloramphenicol

Aminoglycoside

Tetracycline

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)

Lithium: side effects LITH:

Leukocytosis

Insipidus [diabetes insipidus, tied to polyuria]

Tremor/ Teratogenesis

Hypothyroidism

Respiratory depression inducing drugs "STOP breathing":

Sedatives and hypnotics

Trimethoprim

Opiates

Polymyxins

Benzodiazepenes: antidote "Ben is off with the flu":

Benzodiazepine effects off with Flumazenil.

PHARMACOLOGY Mechanisms A. Scopolamine • Anti-muscarinic • Motion Sickness; preoperatively to

reduce secretions • Anti-muscarinic toxicities (mydriasis & cycloplegia; decreased secretions & sweating;
flushing; bradycardia (low doses); tachycardia (high doses); urinary retention; drowsiness, hallucinations,
coma)

Typical Anti-psychotics (Chlorpromazine, Haloperidol, Thioridazine) • Dopamine antagonists •

Schizophrenia; psychosis • Lactation; Extrapyramidal effects (parkinsonism, akathisia (motor
restlessness), tardive dyskinesia (lip smacking, jaw movements, etc.)); anti-cholinergic effects
(antimuscarinic, alpha-antagonistic (orthostatic hypotension), and anti-histamine (sedation)). Toxicities
are a tradeoff—higher extrapyramidal effects coincide with lower anticholinergic effects and vice-versa.
The higher the extrapyramidal effects, the higher the potency (haloperidol > chlorpromazine >
thioridazine)

Atypical anti-psychotics (Clozapine) • Dopamine antagonist • Schizophrenia; psychosis • NO

extrapyramidal effects or lactation; agranulocytosis (fatal); Neuroleptic Malignant Syndrome (catatonia,
autonomic instability, stupor); anti-cholinergic effects as above

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

C. Acarbose • Alpha-glucosidase inhibitor—decreases absorption of glucose • NIDDM; adjunct to insulin

in IDDM • Flatulence; diarrhea; abdominal cramping

D. Losartan • Angiotensin II antagonist • Hypertension • Similar to ACE inhibitors but no cough

(decreased bradykinin activation)

E. Myasthenia Gravis Drugs • Inhibit cholinesterase • Diagnosis (edrophonium); long-term treatment

(Neostigmine, Pyridostigmine); open-angle glaucoma; reversal of non-depolarizing nm blockade •
Fasciculations & weakness

F. Leuprolide • GnRH analog  desensitization of pituitary receptor  decreased FSH, LH secretion •

Prostate Cancer • Transient excess testosterone production (prevent by combining with flutamide);
impotence, hot flashes, tumor flare

G. Flutamide • Blocks inhibitory effects of testosterone on GnRH release • Combo with leuprolide

H. Aminoglutethimide • Inhibits Cholesterol  pregnenelone conversion (like metyrapone) • Metastatic

breast cancer (decreased estrogen) • Induces P450; transient CNS depression; rash
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)
Heparinosteoporosis with chronic use. Thombocytopenia – usually transient and mild. b)
ThiazidesHyperlipidemia, 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 ETOHMetabolized 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).
6) Pharmacogenetics: drugs whose metabolism is affected by inheritance: a) Isoniazid: Most commonly
used drug for the treatment of TB. i) Inhibits biosynthesis of mycolic acids. ii) Metabolized in the liver
(acetylated); speed of acetylation and consequently isoniazid’s half life is genetically determined (fast vs.
slow acetylators). 7. Treatment of Anemia A. Anemia is due to increased destruction or decreased
production. B. Microcytic anemia 1. Iron – absorbed in the duodenum and proximal jejunum. Iron
deficiency seen in premature infants, pregnant and lactating women. Ferrous oral salts can be given; give
for 3-6 months to replenish iron stores. IV iron can also be given. 2. Iron toxicity a. N/V, cramps,
constipation, diarrhea – dose-related so decrease the dose b. Acute toxicity – seen in kids, necrotizing
gastroenteritis followed by shock, lethargy, dyspnea c. Chronic iron toxicity - hemochromatosis C.
Megaloblastic anemia – lack of vitamins needed for normal DNA synthesis, so the RBC gets biggger
(macrocytic) 1. Vitamin B12 (normally obtained in meats), requires intrinsic factor for absorption
(pernicious anemia decreases absorption), gastrectomy also decreases absorption. B12 is stored in the
body (years supply) a. B12 deficiency also shows nervous defects b. B12 shots can be given if oral
absorption is a problem c. Folate will NOT correct neurological features, but WILL help with the anemia
2. Folic Acid – from green leafy veggies, body stores of folate are lower (1-6 months) a. Deficiency
doesn’t have neurological deficits b. Folic acid is well absorbed orally D. Decreased production 1.
Erythropoietin – used for renal failure, bone diseases, chemotherapy a. Toxicity – too rapid increase in
hematocrit can lead to HTN, thrombotic complications 2. Colony stimulating factors (G-CSF, GM-CSF) a.
Increase recovery after myelosuppressive chemotherapy or BMT 8. Prevention/treatment of
cerebrovascular disease K. Aspirin 1. Irreversibly blocks cyclooxygenase, = inhibits thromboxane (TxA2)
formation from platelets 2. Only requires a small daily dose L. Ticlopidine 1. Inhibits platelet aggregation
(inhibits ADP pathway) 2. Decreases TIAs, completed strokes, unstable angina pectoris 3. Diarrhea in
20%, leukopenia in 1% (must monitor white count) M. Thrombolytics – catalyze formation of plasmin, a
generalized lytic state in body is produced 1. Streptokinase – cheap, allergic reactions possible 2.
Urokinase 3. Tissue plasminogen activators (t-PA) – expensive, from recombinant DNA 9. Treatment of
rheumatoid arthritis A. Drugs that alter Pain 1. Aspirin – 1st line drug, GI problems 2. NSAIDS - 3. COX-2
inhibitors – less GI problems B. Drugs that Decrease Progression 1. Methotrexate and
immunosuppressives – more toxic side effects 2. Gold – dermatitis is common side effect 10. Vaccines:
indications, potential side effects A. Indications 1. Active immunization – antigen is given so host
develops antibodies (long protection) a. Give to children 2. Passive – immunoglobins are given (short
term protection) a. Give to those recently exposed (Tetanus, Botulinum, HBV, Rabies) or to travelers
(Polio, tetanus, Measles, diphtheria) B. Side Effects 1. Giving live attenuated vaccines may cause the
disease (eg. Polio vaccine) 2. Killed vaccine will not cause the disease 3. Allergic reactions are possible
11. Chemotherapeutic agents: risk of possible secondary cancer