First AID Pharm

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Penicillin (MOA)

bind pbps, block transpeptidase cross-linking of cell wall, bacteria autolysin activity

Methicillin (toxicity)

interstitial nephritis

Ampicillin, Amoxicillin (clinical use)

Gram + and H. influenza, E. coli, Listeria, Proteus, Salmonella and enterococci

Ampicillin (toxicity)

pseudomembranous colitis

Ticarcillin, carbenicillin, pipercillin (clinical use)

Pseudomonas and gram - rods
use with clavulanic acid

B-lactamase inhibitors

clavulanic acid, sulbactam, tazobactam
used in combo with antipseudomonals and aminopencillins

Bacteriostatic

Erthromycin, Clindamycin, Sulfamethoxazole, Trimethoprim, Tetracyclines, Chloramphenicol

Bacteriocidal

Vancomycin, Fluoroquinolones, Pencillin, Aminoglycosides, Cephalsporins, Metronidazole

Cephalosporins (MOA)

B-lactam drugs that inhibit cell wall synthesis but less suspectible to penicillins

1st generation Cephs (names and clinical use)

Cefazolin, Cephalexin
Gram + and Proteus, E. coli, Klebsiella

2nd generation Cephs (names)

Cefaclor, Cefoxitin, Cefuroxime, Cefamandole
(its a FACt i want a FOXy FURy MAN)

2nd generation Cephs (clinical use)

HEN PEcKS
H. influenza, Enterobacter, Neisseria, Proteus, E. coli, Klebsiella, Serratia

3rd generation Cephs

Ceftriaxone, Cefotaxime, Ceftazidine
Cross the BBB
Covers serious gram - except LAMEs (Listeria, Atypical, MRSA, Enterococci)

4th generation Cephs

Cefepime
covers Pseudomonas and gram +

Cephs (toxicity)

Nephrotoxicity with aminoglycosides
disulfram like reaction

Aztrenam (clinical use)

Gram - rods
DOES NOT WORK ON gram + or anaerobes
No cross-sensitivity with pens and cephs

Imipenem/cilastatin (MAO)

B-lactamase resistant carbapenem.
Cilastatin inhibits dihydropeptidase I in the kidney

Imipenem and Meropenem (clinical use)

Broadest spectrum
used empiric therapy
DOC for Enterobacter

Vancomycin (MAO and clinical use)

inhibits cell wall mucopeptide formation by binding D-ala D-ala
used for MRSA and multidrug resistant gram +

Vancomycin (Resistance)

amino acid change from D-ala to D-lac

Vancomycin (Toxicity)

Nephrotoxicity, Ototoxicity, Thrombophlebitis, RED MAN SYNDROME

30S inhibitors

Aminoglycosides
Tetracylcines

50S Inhibitors

Chloramphenicol, Clindamycin
Erythromycin
Lincomycin
Linezolid

Aminoglycosides (names and MAO)

Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin
inhibit initiation complex and cause misreading of mRNA

Aminoglycosides (clinical use and toxicity)

MUST HAVE OXYGEN--> ineffective against anaerobes
use for gram - rods
Nephrotoxicity, Ototoxicity, Neuromuscular blockade, Teratogen

Aminoglycosides (resistance)

transferase enzyme or enzymes that inactivate by adenylation, acetylation, and phosphorylation

Tetracyclines (MAO)

prevent attachment of aminoacyl tRNA
DON'T take with milk or iron due to divalent cations which inhibits absorption

Tetracyclines (clinical use)

Vibrio chlorea, acne, Chlamydia, Ureaplasma, Mycoplasma, H. Pylori, Borrelia, Rickettsia

Tetracylcine (toxicity)

teeth discoloration, inhibition of bone growth, photosensitivity

Macrolides (names and MAO)

ACE (azithromycin, clarithromycin, erythromycin)
inhibits protein synthesis by blocking translocation by binding 23S rRNA of the 50S

Macrolides (clinical use)

Mycoplasma, Legionalla, Chlamydia, Neisseria

Macrolides (toxicity)

Prolonged QT interval, GI discomfort, acute cholestatic hepatitis

Chloramphenicol (MAO and clinical use)

inhibits 50S peptidyltransferase
Meningitis

Chloramphenicol (toxicity)

Aplastic anemia
Gray baby syndrome due to lack of UDP-glucuronyl transferase

Clindamycin (MAO)

blocks peptide bond formation at 50S ribosomal subunit

Drugs used for VRSA

Streptogramins (quinupristin/dalfopristin)
Linezolid

Sulfonamides (MAO)

PABA antimetabolite
inhibits dihydropteroate synthetase

Sulfonamides (toxicity)

hemolysis in G6PD deficiency
nephrotoxicity
photosentivity
kernicterus due to displacement of bilirubin

Trimethoprim (MAO and toxicity)

inhibits bacterial dihydrofolate reductase
toxicity: megaloblastic anemia, leukopenia, granulocytopenia

Polymyxins (MAO)

bind to cell membranes of bacteria and disrupt their osmotic properties
cationic, basic proteins that act like detergents

Polymyxins (clinical use and toxicity)

used for resistant gram - infections
neurotoxicity, acute tubular necrosis

Ethambutol (MAO)

inhibits arabinosyl transferase which polymerizes arabinose into arabinoglactan

Ethambutol (toxicity)

red green color blindness

Rifampin (MAO)

inhibits DNA-dependent RNA polymerase

Rifampin (toxicity)

hepatotoxicity, P-450 inducers, orange body fluids
DON'T USE with HIV patients bc affects mitochondrial synthesis of RNA

Tetracycline (resistance)

PUMP
decrease uptake or increase transport out of cell

Macrolides (resistance)

methylation of rRNA

Azoles (MAO)

inhibit fungal sterol synthesis (blocks 14-alpha-demethylase)

Flucytosine (MAO and toxicity)

inhibits DNA synthesis by conversion to 5-fluorouracil
bone marrow suppression

Caspofugin (MAO and clinical use)

inhibits cell wall synthesis by inhibiting synthesis of B-glucan
used for invasive aspergillosis

Terbinafine (MAO and clinical use)

inhibits squalene epoxidase
used to treat dermatophytoses

Griseofulvin (MAO)

interferes microtubule function; disrupts mitosis

Griseofulvin (clinical use and toxicity)

dermatophytoses (oral treatment)
P-450 inducer, teratogenic, carcinogenic

Amantadine (MAO)

blocks viral penetration/uncoating
M2 protein

Amantadine (clinical use and toxicity)

Influenza A and Parkinson's disease
toxicity: ataxia, slurred speech, dizziness (DRUNK)

Zanamivir, Oseltamivir (MAO)

inhibit influenza neuraminidase

Acyclovir (MAO)

Inhibits DNA synthesis in HSV, VZV, and EBV. Activated by viral thymidine kinase (TK- strains are resistant).

Acyclovir (toxicity)

crystalline nephropathy

Ganciclovir (MAO)

Inhibits DNA synthesis. Effective against herpes viruses CMV and HSV; for CMV requires bioactivation via viral phosphotransferase.

Ganiciclovir (toxicity)

leukopenia, neutropenia, thrombocytopenia, renal toxicity

Foscarnet (MAO)

Viral DNA polymerase inhibitor that binds to the pyrophosphate-binding site of the enzyme. Does not require activation by viral kinase.
PYROPHOSPHATE ANALOG

Foscarnet (clinical use and toxicity)

Uses: CMV retinitis in immunocomp pts. when gancyclovir fails. Tox: Nephrotoxicity

Protease Inhibitors (-navir) (MAO)

inhibit maturation of new virus by blocking protease in progeny virus
ritonavir P450 inhibitor

Protease Inhibitors (toxicity)

GI intolerance, hyperglycemia, kidney stones, thrombocytopenia

NRTI (names)

Zidovudine, Abacavir, Didanosine (ddI), Lamivudine (3TC), Stavudine (d4T), and Zalcitabine (ddC

NNRTI (names)

Efavirenz, Declaviridine, Nevirapine

Reverse transcriptase inhibitors (MAO)

inhibit reverse transcriptase of HIV
inhibits 5' -->3' phosphodiester linkage formation

Reverse transcriptase inhibitors (toxicity)

bone marrow suppression, peripheral neuropathy, lactic acidosis (NRTI), rash (NNRTI)

Enfuviritide (MAO)

bind viral gp41 subunit
inhibit conformational change required for fusion with CD4 cells
BLOCK VIRAL PENTRATION

Maraviroc (MAO)

blocks CCR5 protein on T-cell surface to prevent viral entry

Interferons (MAO)

Glycoproteins synthesized by virus-infected cells block replication of both RNA and DNA viruses

Interferon alpha

used in hep B and C, kaposi's sarcoma

interferon beta

Multiple sclerosis

interferon gamma

NADPH oxidase deficiency

Praziquantel (MAO and clinical use)

Increases membrane permeability to Ca2+ causing muscle contraction followed by paralysis.
Used for flukes and tapeworms

Ivermectin (MAO)

Intensifies GABA-mediated neurotransmission in nematodes, but no access to CNS in humans.

Mebendazole (MAO)

Inhibits microtubule synthesis and glucose uptake in
nematodes

Sodium Stibogluconate (MAO)

Inhibits glycolysis at PFK reaction. Used against LESHMANIA DONOVANI.

Nifurtimox (MAO and clinical use)

Forms intracellular oxygen radicals, which are toxic to the organism. Used against TRYPANOSOMA CRUZI.

Cyclosporine (MAO)

inhibits calcineurin --> prevents production of IL-2 and its receptor

Cyclosporine (toxicity)

nephrotoxic, gingival hyperplasia, hirtuism

Tacrolimus (FK506) MAO

binds to FK-binding protein --> inhibiting secretion of IL-2

Azathioprine (MAO)

precursor of 6-mercaptopurine
interfers with metabolism and synthesis of nucleic acids

Muromonab-CD3 (OKT3) MAO

monoclonoal antibody that binds to CD3 on the surface of T cells

Sirolimus (MAO

blocks tyrosine kinase. binds to mTOR.
inhibit T-cell proliferation in response to IL-2

Clinical use for Aldesleukin (interleukin2)

renal cell carcinoma
metastatic melanoma

Clinical use for erythropoietin

Anemia esp in renal failure

alpha 1 receptor

increase vascular smooth muscle contraction, pupil dilator muscle (mydriasis), increase intestinal and bladder sphincter muscle contraction, decrease renin release

alpha 2 receptor

decrease insulin release, decrease sympathetic outflow

Beta 1 receptor (heart and kidney)

increase HR, contractility, renin release

Beta 2 receptor

vasodilation, bronchodilation, increase heart rate and contractility, increase insulin release, decrease uterine tone

M2 (heart)

decrease HR and contractility of atria

M3 (peripheral)

increase exocrine gland secretions, miosis, accommodation

Bethanechol

Cholinomimetic. Activates bowel and bladder smooth muscle. Resistant to AChE. Uses: Postoperative and neurogenic ileus and urinary retention

Carbachol

Cholinomimetic. ACh analog. Uses: Glaucoma, pupillary constriction, and relief of intraocular pressure.

Pilocarpine

Cholinomimetic. Contracts ciliary muscle of eye (open angle), pupillary sphincter (narrow angle). Resistant to AChE. Uses: Glaucoma, Sjoren, Stimulator of tears, sweat, and saliva.

Neostigmine

Cholinesterase inhibitor. Increase endogenous ACh. Little CNS effect. Uses: Postoperative ileus and urinary retention, MG, reversal of neuromuscular blockade.
DON'T ENTER CNS

Physostigmine

Glaucoma, crosses BBB. atropine overdose

DUMBBELSS

Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, Salivation.
Antidote: Atropine + pralidoxime

Muscarnic antagonists

Atropine, Benztropine, Scopolamine, Ipratropium, Oxybutyin, Methscopalamine

Atropine

Blocks DUMBBELSS
toxicity: "red as a beet, dry as a bone, blind as a bat, mad as a hatter, hot as a hare"

Don't use Atropine in ...

acute angle glaucoma in elderly
urinary retention
hyperthermia in infants

Hexamethonium

Nicotinic antagonist (blocks para and sympathetic). Uses: Ganglionic blocker. In experimental models, prevents vagal reflex responses to changes in blood pressure - prevents reflex brady.

Hexamethonium (toxicity)

Tox: Orthostatic Hypotension, Blurred vision, constipation, sex dysfunction

Epinephrine (MAO)

Direct sympathomimetics. affinity for all receptors. low doses (B1), high doses (alpha1).

Epinephrine (clinical use)

anaphylaxis, glaucoma (open angle), asthma, hypotension

Epinephrine (toxicity)

tachycardia, hypertension, MI, pulmonary edema and hemorrhage

Norepinephrine (MAO)

Adrenoceptor agonist prototype: acts at B1- and all A adrenoceptors
increase BP, TPR, HR and pulse pressure

Norepinephrine (clincal use and toxicity)

hypotension
Tox: ischemia, arrhythmias, HTN, reflex bradycardia.

Isopropterenol (low dose epi)

B1 and B2 agonist catecholamine prototype: bronchodilator, cardiac stimulant. Always causes tachycardia because both direct and reflex actions increase HR. Tox: arrhythmias, tremor, angina.

Dopamine

Neurotransmitter and agonist drug at dopamine receptors: used in shock to increase renal blood flow (low dose) and positive inotropic effects (moderate dose).

Dobutamine

b1>b2
increase HR, contractility, conduction velocity and myocardial oxygen consumption

Dobutamine (clinical use)

shock, heart failure, cardiogenic shock

Phenylephrine

A1 > A2. Uses: Pupillary dilation, vasoconstriction, nasal decongestion

B2 selective agonist

Metaproterenol, Albuterol, Salmeterol, Terbutaline

Nonselective alpha blockers

Phenoxybenzamine (irreversible)
phentolamine (reversible)
Used in pheochromocytoma. Tox: excess hypotension; GI distress.

Prazosin, Terazosin, "-osins"

Alpha1-selective blocker prototype: used in HTN and benign prostatic hyperplasia. Tox: first-dose orthostatic hypotension but less reflex tachycardia than nonselective a blockers.

Alpha 2 blockers

Mirtazapine (depression) and Yohimbine
Tox: sedation, increase serum cholesterol and appetite

(Inducers) Queen Barb Steals Phen-phen and Refuses Greasy Carbs Chronically

Quinidine, Barbiturates, St. John's wort, Phenytoin, Rifampin, Griseofulvin, Carbamazepine, Chronic alcohol use
metabolized faster where it doesn't work

(Inhibitors) Inhibit yourself from drinking beer from a KEG because it makes you Acutely SICk

Sulfonamides, Isoniazid, Cimetidine, Ketoconazole, Erythromycin, Grapefruit juice, Acute alcohol use

HMG-CoA reductase inhibitors (MAO)

inhibit cholesterol precursor, upregulates LDL receptors

HMG-CoA reductase inhibitors (toxicity)

hepatitis
myopathy (rhabdomyolysis)

Niacin (MAO)

inhibits lipolysis in adipose tissue.
reduces hepatic VLDL secretion into circulation

Niacin (toxicity)

flushed skin (decresed by aspirin)
hyperglycemia
hyperuricemia
hepatitis

Bile acid resins (cholestyramines)

Prevent intestinal reabsorption of bile acids. Liver must use cholesterol to make more

Bile acid resins (toxicity)

GI discomfort, decrease absorption of fat-soluble vitamins. GALLSTONES

Fibrates (MAO)

upregulate LPL--> increase in TG clearance

Fibrates (toxicity)

myositis
heptptoxicity
GALLSTONES

Hydralazine

Antihypertensive. Arteriolar vasodilator, orally active. Uses: Severe HTN, CHF, HTN in preg (with Methyldopa). Metabolized by Acetylation. Tox: Tachycardia, Salt and H2O retention, Lupus like syndrome.

Minoxidil

K+ channel opener that hyperpolarizes and relaxes vascular smooth muscle. Uses: Severe HTN, baldness. Tox: Hypertrychosis, Pericadial effusion, Reflex tachy, Angina, Salt retention.

Nifedipine

Dyhydropiridine calcium channel blocker. Vasoselective (N>D>V). Uses: Hypertension, Angina, Printzmetal's angina, Reynaud's. Tox: Cardiac depression, AV block, edema, flushing, dizziness, constipation.Others: Amlodipine (HF), Nimodipine (subarachnoid hemmorhage), Nicardipine

Fenoldopam

D1 receptor antagonist. Relaxes smooth muscle. Powerful vasodilator. Uses: Hypertensive emergencies

Digoxin

Cardiac glycoside. Direct inhibitor of Na+/K+ pump leading to indirect inhibition of Na+/Ca++ exchanger and increasing intracellular calcium levels. Stim. vagus. T1/2 40hrs. Uses: CHF, A-fib. Tox: Calcium overload arrhythmias, GI upset.

Class 1A antiarrhythmic
Quinidine, Procainamide, Disopyramide

. Uses: Atrial and vetricular arrhythmias. Tox: Cinchonism - headache, tinnitus, Thrombocytopenia, Torsades. Others: Procainamide, Dysopyramide. Increase AP

Class 1B antiarrhythmic.
Lidocaine, Mexiletine, Tocainide

Selectively affects ischemic or depolarized vent. tissue. Uses: Acute V-arrhythmias (post MI) and digoxin tox. Tox: Local anesthetic, CNS stim/ dep, cardiovascular depression. Others: Mixeiletine (Oral), Tocainide. Decrease AP

Class 1C antiarrhythmic
Flecainide, Encainide, Propafenone

Class 1C antiarrhythmic. No effect on AP. Uses: V-tach and rapid SVT with WPW. Tox: Proarrhythmic (post MI), Prolongs refractory period in AV. Others: Encainide, Propafenone

Adenosine

Unclassified antiarrhythmic. Parenteral only. Hyperpolarizes AV nodal tissue causing block for 10 - 15 secs. Very short acting. Uses: Drug of choice in abolishing/ diagnosing SVT. Tox: flushing, hypotension, chest pain

Mg++

Effective in torsades de pointes and digoxin toxicity.

Lispro, Aspart, Regular Insulin

Short acting insulin analogs. Bind insulin receptor (TK). Liver - Increase glucose stored as glycogen. Muscle - Increase glycogen and protein synthesis, K+ uptake. Fat - Aids TG storage. Uses: DM1, DM2, Hyper K+. Tox: Hypoglycemia

NPH

Intermediate acting insulin analog. Bind insulin receptor (TK). Liver - Increase glucose stored as glycogen. Muscle - Increase glycogen and protein synthesis, K+ uptake. Fat - Aids TG storage. Uses: DM1, DM2, Hyper K+. Tox: Hypoglycemia

Glargine, Detemir

Long acting insulin analogs. Bind insulin receptor (TK). Liver - Increase glucose stored as glycogen. Muscle - Increase glycogen and protein synthesis, K+ uptake. Fat - Aids TG storage. Uses: DM1, DM2, Hyper K+. Tox: Hypoglycemia

Sulfonlyureas

Blocks K+ channels in pancreatic B cells, causing depolarization and release of insulin. Uses: Only DM2. Tox: hypoglycemia, weight gain, cholestatic jaundice

Metfomin

Oral biguanide hypoglycemic. Decreases hepatic gluconeogenesis, Increase Glycolysis, and peripheral glucose uptake (insulin sensitivity). Uses: Oral, can be used in DM1. Minimal hypoglycemia or weight gain. Tox: Lactic acidosis. DON'T use in renal failure

Pioglitazone, Rosiglitazone

peroxisome proliferator-activator receptors (PPARs) enhances target tissue sensitivity to insulin.
Uses: DM2. Tox: weight gain, edema, hepatotoxicity, cardiotoxicity

Acarbose, Miglitol

Alpha-glucosidase inhibitors. Delayed sugar hydrolysis and glucose absorption leads to decreased postprandial hyperglycemia. Uses: DM2. Tox: GI disturbances.

Pramlintide

Mimetic.(amylin analog) Decreases glucagon release. Uses: DM2. Tox: Hypoglycemia, nausea, diarrhea

Exenatide

GLP-1 analog. Increased insulin, decreased glucagon release. Uses: DM2. Tox: Nausea vomiting, pancreatitis, weight loss

Propylthiouracil, Methimazole

Antithyroid drug. Inhibits tyrosine iodination and coupling reactions. Orally active. Uses: Hyperthyroidism. Tox: Rash, agranulocytosis (rare). Methimazole is a possible teratogen

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