Pharmacology Final

Parasympathetic

Bethanechole → Pee, Atropine antidote

Neostigmine and Physostigmine → M. Gravis, Alzheimers, glaucoma

Sympathetic

Atropine → No pee

Glycopyrrolate → Pre-anesthetic

Scopolamine → Motion sickness

Natural Sympathetic: Epinephrine (EpiPen, Anaphylaxis), norepinephrine, dopamine (increase BP) antidote → Phentolamine

Sympathetic synthetic → Isoproterenol, Dobutamine

Albuterol → Asthma

Beta-1+2

Beta 1 - Increase Heart Rate

Beta 2 - Lungs, Uterus: dilate/relax → hyperglycemia

Dopamine

Kidney perfusion, for shock/renal failure → Antidote Phentolamine, activates B1

Beta-Blockers

1st gen (nonselective), propranolol, peripheral, lower HR, stage right, migraines, hyperglycemia

2nd gen (selective), metoprolol, B1, Lower HR, BP, and raises Sugar/glucose

Potassium

3.5-5

Hypokalemic - Narrow and flat, infuse slowly 10

Hyperkalemic - Long, Tented, wide, depressed

pH balance 7.35-7.45

Acidosis: High H+, K+, low pH, Hypoventilation, Sodium bicarbonate

Alkalosis: Low H+, K+, high pH, hyperventilation, Chloride

Diuretics for HTN

Loop, Furosemide, Ototoxicity

Thiazide, 1st, no pregnancy

Potassium-sparing, Spironolactone

Osmotic, Mannitol, brain swelling

Carbonic anhydrase inhibitor, altitude sickness

LDL Cholesterol HTN -statins

HMG-CoA blocker, take at dinner or bedtime, watch for myopathy, muscle pain, and liver

CO + BP equations, Preload and Afterload

BP = CO x SVR

CO = SV x HR

Preload - Veins, dilated = decreased

Afterload - Arteries, dilated = decreased

Antihypertensive Medications

Calcium Channel Blocker

Nifedipine - Dihydropyridine, arteries, peripheral.

Verapamil - Non-dihydropyridine, constipation and digoxin toxicity.

Diltiazem - Non-dihydropyridine, (hyperplasia)

Vasodilator

Hydralazine - Orthostatic hypotension, arteries.

Minoxidil - Hair growth, arteries.

Sodium Nitroprusside - Veins and arteries, rapid.

Alpha-1 blocker

Prazosin - selective, blood vessels and eyes, watch for orthostatic hypotension.

Phentolamine - Non-selective, blood vessels and eyes, watch for orthostatic hypotension.

Alpha-2 inducer

Clonidine - brain, CNS, lowers BP, HR, ADHD, pain.

Natural BP

Cardiovascular - Norepinephrine

Kidneys - Renin-RAAS system

Aliskiren - Renin

-pril, ACE inhibitors, Angiotensin I, decreases it, watch for angioedema

-sartan, ARBs, Blocks Angiotensin II (powerful one), no pregnancy

Aldosterone, Spironolactone, Eplerenone, hyperkalemia

Antianginal & Antidysrhythmic Medications

Nitroglycerin: Angina: 1 dose (not working; call 911), 3 times, 5 minutes apart, Sublingual, rapid; watch for headache; drug holiday; sildenafil and PDE5: watch for hypotension, Reflex tachycardia

Digoxin: Glycoside for antidysrhythmic, 0.5–0.8 narrow therapeutic range, HR below 60: notify provider, don't give, Toxicity if hypokalemia and Verapamil, watch for nausea/vomiting, dysrhythmia, and yellow halos

Lidocaine: Ventriculars, bottom of heart, Sodium, for antidysrhythmia, monitor ECG

Amiodarone: Potassium for antidysrhythmia, Ventricular, Severe toxicity, blindness, cough, chest pain, long ½ life

Adenosine: Flatline, Methyl and caffeine block effect

Atrial & Ventricular Dysrhythmias

Atrial: work on antidysrhythmia: Beta blocker: -prolol, Calcium: Verapamil and Diltiazem

Works on Ventricular: Sodium – Lidocaine, Potassium – Amiodarone

Anticoagulants & Antiplatelets

Anticoagulants: Prevent DVT, no fibrin/scabbing

Heparin: Antithrombin anticoagulant, not PO, rapid, large and charged, aPTT testing, Antidote: protamine sulfate, HIT – 50% platelet drop or below 100,000 platelets: stop heparin, contact provider, for long DVT

Enoxaparin/Lovenox: Anticoagulants, antithrombin, SubQ, fixed, at home, Long half-life, Better than Heparin, but expensive

Warfarin: Vitamin K anticoagulant, PO, PT/INR = 2–3, No pregnancy, Genetic: VKORC1, CYP2C9, Vitamin K increase dose

Dabigatran: Direct thrombin inhibitor, Anticoagulant, PO, rapid, Fewer drug interactions than warfarin, Antidote → Idarucizumab

Rivaroxaban: Xa factor, PO, rapid, fixed, Anticoagulant

Aspirin and Clopidogrel: Antiplatelets, No stick, Daily MI and clots, Watch for GI bleeding and epidural hematoma

Clopidogrel: P2Y12 inhibitor, Prevents platelet aggregation, Used after stent, Prodrug, Monitor for bleeding, TTP

Thrombolytics, Heart Failure & Types of Thrombi

Alteplase (tPA) and Tenecteplase (TNK): Clot busters, thrombolytics, Emergencies, Ischemic stroke, not hemorrhagic stroke, STEMI, Major risk for severe bleeding, IV sites and clots, watch for headache

tPA: IV, short ½ life, rapid

TNK: More fibrin-specific and longer half-life

Heart Failure Drug Recipe

• Diuretics – edema

• RAAS – lower BP

• Beta blockers – HR

• Digoxin (slow and strong)

Arterial Thrombi: Aspirin and Clopidogrel, MI, Stroke, Stent

Venous Thrombi: Anticoagulants, DVT, Pulmonary

Endocrine/Thyroid

Anterior Thyroid - TSH, Hypothyroidism, Goiter, Coma

Posterior Thyroid - TRH, stimulated from Hypothalamus

TSH regulated by T3 (Triiodothyronine) - Hyperthyroidism/Graves

T4 (Thyroxine) - dysfunction

Thyroid regulates heart, energy, and growth

Hypothyroidism/Goiter/Coma

Levothyroxine

Increases T4, decreases TSH

1 month until therapeutic effect; lifelong treatment

Take on an empty stomach

Half-life: 1 week

Increases: CYP inducers, sertraline, warfarin, catecholamines (epinephrine, dopamine, dobutamine)

Inhibits absorption: H2 blockers, iron, magnesium, calcium, sucralfate

Hyperthyroidism + Graves

1) Methimazole - Thyroidectomy or thyroid storm; avoid during pregnancy, especially during the first trimester. Monitor for agranulocytosis (report fever, sore throat, or signs of infection).

2) Radioactive Iodine - Use precautions around household contacts. Mild toxicity: Metallic or brassy taste, mouth sores. Severe toxicity: GI distress.

Growth Hormone

Somatropin (IV or SubQ): short stature, Prader-Willi syndrome.

AE: hyperglycemia, glucocorticoid interactions

Toxicity Acromegaly, pre-puberty: Gigantism.

Antidiuretic Hormone (ADH), Hypothalamic, Diabetes Insipidus

Vasopressin – Natural ADH - Cardiovascular effects: increased BP, vasoconstriction, angina/MI, gangrene.

Desmopressin – Synthetic ADH - More routes, longer duration, weak pressor agent, fewer cardiovascular adverse effects.

Risk of water toxicity; monitor fluid intake and follow fluid restrictions. Caution with diuretic therapy.

Diabetes

HbA1c: ≥ 6.5%

Fasting BG: ≥ 126 mg/dL (on 2 separate occasions)

OGTT: ≥ 200 mg/dL (2 hours after glucose intake)

Random blood glucose + symptoms: ≥ 200 mg/dL

Symptoms: Polyuria, Polydipsia, Polyphagia

Short-Term - Diabetic Ketoacidosis Type 1, Hyperosmolar Hyperglycemic State Type 2

Long-Term - CVD, Retinopathy, Nephropathy, Gastroparesis, infections, and amputations

Hypoglycemia + Hyperglycemia

BG: <70 mg/dL; decreased carbohydrate intake, increased insulin, or exercise.

Symptoms: Sweating, shakiness, confusion, dizziness, or loss of consciousness.

Treatment (15-15 rule): Check BG, Consume 15 g of fast-acting carbohydrates, Recheck BG after 15 minutes, Repeat if BG is still below 70 mg/dL, If hypoglycemia persists despite treatment, seek emergency medical care.

Severe hypoglycemia: Glucagon if the patient cannot safely swallow or is unconscious; Stimulates the liver to release stored glucose (glycogenolysis) and make new glucose (gluconeogenesis), rapidly raising BG.

Hyperglycemia: BG: >180–220 mg/dL, Increased carbohydrate, decreased insulin, or stress.

Polyuria, polydipsia, polyphagia, headache, and altered mental status.

Insulin

Glucose into cells.

AEs: Hypoglycemia, lipohypertrophy (fat buildup)

Rapid-acting: Glulisine, aspart, lispro.

Short-acting: LIN

Intermediate-acting: NPH (cloudy) N

Long-acting: Glargine, detemir, basaglar.

Ultra-long-acting: Degludec

NPH insulin can be mixed with rapid or short-acting insulin

Beta Blockers mask; glucocorticoids & sympathomimetics increase BG; counteract insulin

T2DM Drugs

Biguanides/Metformin decrease hepatic/liver glucose production & increase glucose uptake by muscle/tissue for T2DM, prediabetes, gestational diabetes, PCOS. AE: GI, decreased B12 absorption, lactic acidosis. Interactions: Alcohol, cimetidine, iodinated contrast media.

Sulfonylureas/Glyburide: stimulate the pancreas to release insulin; T2DM. Interactions: Beta blockers, alcohol, and insulin. AE: Hypoglycemia and weight gain.

GLP-1’S

Exenatide & Semaglutide

GI hormone; increases glucose-dependent insulin release, decreases glucagon

Slow gastric emptying, decreases appetite

For: T2DM and weight loss.

AEs: GI, pancreatitis, thyroid C-cell tumors, hypoglycemia

Inflammation

Nonspecific response to tissue injury or microorganisms. Arthritis most common

Cardinal Signs:

Rubor, Calor (heat), Tumor, Dolor/Pain, Functio laesa

Immunity

Innate: Nonspecific defense.

Adaptive: Antigen-specific defense.

Cell-Mediated: T cells and macrophages.

Humoral: B cells, antibodies → specific antigens

Inflammatory Pathway

Tissue damage → Phospholipase A₂ releases arachidonic acid from the phospholipid bilayer.

Arachidonic acid is converted into prostaglandins or leukotrienes.

COX-1: Gastric mucosal protection, renal blood flow, and platelet aggregation.

COX-2: Inflammation, pain, fever, airway function/bronchoconstriction.

NSAIDS & Acetaminophen (APAP) for Prostaglandin

NSAIDs: Aspirin (ASA), ibuprofen, naproxen - decrease prostaglandin synthesis; reduce pain, fever, and inflammation—AEs: GI ulcers, bleeding, kidney damage, fluid retention, HTN. Take with food; do not crush/chew capsules or extended-release forms. Stop before surgery.

Acetaminophen (APAP)/Tylenol - Reduces pain and fever by inhibiting prostaglandin synthesis primarily in the CNS; no anti-inflammatory effect, not an NSAID. Dose: 500–1,000 mg per dose. Maximum adult daily dose: 4,000 mg. Toxicity: N/V, liver failure, death; antidote: N-acetylcysteine.

Selective COX-2 Inhibitor

Celecoxib - Lower risk of GI ulcers + bleeding; minimal effect on platelet aggregation.

Cardiovascular thrombotic events: heart attack & stroke

Corticosteroids

Glucocorticoids (-sone / -solone) (Adrenal/kidney)

Inhibit phospholipase A₂, reduce inflammation

AEs: Immunosuppression, glucose intolerance, Cushing, mood changes, insomnia, cataracts, and peptic ulcers.

Take with food; monitor BG, infection, fluid/electrolyte; use the lowest effective dose for the shortest duration possible; taper

Immunosuppressants and Immune Stimulants

Suppresses T & B cells for organ transplant rejection & autoimmune diseases; risk of infections & neoplasms; avoid grapefruit juice

Stimulants - Interferons/Interleukins (Alfa-2) AE’s: Flu-like symptoms; encourage hydration

Vaccinations

Teach boosters; do not routinely premedicate with acetaminophen or ibuprofen

Aspirin: not for kids/teens → Reye syndrome.

Natural Active: Infection; Natural Passive: Placenta or breast milk

Artificial Active: Vaccination; Artificial Passive: Antibodies, Immune globulin

Microcytic anemia

MCV: <80 fL, Iron: <30 mcg/dL, Ferritin: <20 ng/mL

Take Ferrous iron (Fe²⁺), Oral GI irritation, nausea, and constipation. Empty stomach for better absorption, or with food if GI upset occurs. Avoid taking HS. Use a straw and the back of the tongue for liquid iron (tooth staining) IV/IM Iron — test dose; Z-track, prevent stain

Anemia (acute or chronic)

Blood loss, low production, increased destruction (Sickle cell, thalassemia, sepsis)

B12 Megaloblastic anemia / nerve damage (myelin)

Vitamin B12 (Cobalamin): Animal products.

Pernicious Anemia: Intrinsic factor (absorption) deficiency

Cyanocobalamin (vitamin B12), orally (high-dose, 1,000–2,000 mcg/day); injection if intrinsic factor problem

Folate Megaloblastic anemia

Folic Acid (B9) - Amino acid & DNA synthesis → Fetal neural tube defects; 400 mcg/day; pregnant women need a higher dose. Avoid alcohol.

Check vitamin B12 before treating folate-deficiency anemia; folic acid can correct anemia while allowing B12-related nerve damage to progress

Erythropoietin

RBC (oxygen transport) in the bone marrow.

For: Anemia, CKD, chemo, HIV; CKD: avoid Hgb >11 g/dL

AE: HTN, headache, seizures, thrombosis (blood clots).

Monitor Hgb, BP, CBC, iron. Use the lowest effective dose.

Thrombopoietic Growth Factors

Platelet production in the bone marrow

Oprelvekin: prevents severe thrombocytopenia post-chemo

AEs: Fluid retention, arrhythmias, thrombosis

Nursing: Monitor platelets, fluid, and cardiac/renal function

Leukopoietic Growth Factors

WBC/neutrophils production for neutropenia post-chemo: engulfing/destroying microbes (improves within 1-3 days)

AE: Bone pain and leukocytosis (excessive WBC)

Nursing: Monitor CBC & ANC

Oncology/Chemotherapy drugs PPE

G₀ phase: Resting phase; cells are not dividing, less susceptible to chemotherapy. Chemotherapy damages bone marrow, hair follicles, GI tract cells → Alopecia, neurologic changes, decreased immunity, mouth sores

Hold Medication if Labs Are Low: Anemia, Leukopenia, Neutropenia: neutrophil nadir- the lowest absolute neutrophil count (ANC) reached after chemotherapy-induced bone marrow suppression; Thrombocytopenia: Low platelet count and increased bleeding risk.

Before chemotherapy: antiemetics; monitor baseline CBC, renal/liver function

Eat small, frequent meals; maintain hydration, monitor intake/output, weight; oral hygiene; plan rest, sun protection; monitor BG; avoid aspirin

Anesthetics and Adjuncts to Anesthesia

Local - Lidocaine patch (sodium)

Neuromuscular Junction Blocking Agents

Depolarizing - Succinylcholine, Non-depolarizing others

Analgesics (Pain Meds)

Opioids - Agonists (Morphine), Partial agonists, Antagonists (Naloxone)

Drugs for Headache Management

Abortive (Triptans & Ergot Alkaloids), Preventative

Local Anesthetics (Nurses) w/ Epi

Blocks impulse transmission along axons/pain impulses/sodium channels/action potentials; no LOC; regional anesthesia; loss of sensation. Combined w/ epinephrine; vasoconstriction for bleeding.

Pain → Temp → Touch → Proprioceptio/position→ Skeletal muscle tone (motor). Gain back in opposite order

Amides - Lidocaine (medical) allergic reactions rare

Esters - Dental - hypersensitivity, not effective topically

AE’s: Cardiac and CNS risks, self-inflicted injury; No epi on fingers, toes, nose, and hose

General Anesthesia (Doctors)

Inhalation Anesthetics: Volatile Liquids (Malignant hyperthermia), Nitrous Oxide

IV Anesthetics: Benzodiazepines (GABA), Propofol, Ketamine (psychological reactions)

MOA: Not fully understood

AE’s: Hypotension, respiratory depression; monitor VS, ECG, resuscitation equipment

Balance Anesthesia - Multiple drugs for lower, safer doses

Adjuncts to Anesthesia - Complement drugs for anxiety, N/V

Neuromuscular Junction Blocking Agents (Rare)

Muscle Paralysis without LOC (BBB), hearing/thinking intact

Depolarizing - Succinylcholine/ACh (Malignant hyperthermia)

Non-depolarizing - Pancuronium “-rium” antagonists to ACh

Side Effects: Respiratory arrest, diaphragm paralysis, hypotension, muscle pain, monitor VS, ECG, protect skin

Indications: Muscle relaxation, electroshock therapy

Malignant Hyperthermia from (Succinylcholine, volatile gas)

Early signs: Muscle rigidity, metabolic acidosis (more CO2), dysrhythmias, hypoxia, hypermetabolism

Late: Fever, cyanosis, hypotension, seizures, fatal

Rescue: Dantrolene, ICU, (autosomal dominant educate)

Analgesic (Pain) Medications

Opioids (Combined with non-opioids)

Agonists - Morphine, mu & kappa, cross the BBB (don’t use with head trauma) and the placenta

Partial Agonists - Butorphanol, low potential for abuse

Antagonists/reversal - Naloxone, blocks mu & kappa, may require several doses

AE: GI slows, sedation, respiratory depression, orthostatic hypotension, urinary retention, cough suppression, LOC, miosis, pinpoint pupils

Headache/Migraine Drugs

Abortive/Serotonin Agonists: Triptans, Ergot Alkaloids

Sumatriptan: first-line serotonin (5-HT1) antagonist; vasoconstriction; side effects: paresthesia, chest pressure, vasospasms; teratogenesis; monitor V/S; separate from ergot alkaloids by 24 hours; separate from MAOIs/SSRIs

Second-line migraine-specific: stimulate alpha-adrenergic receptors, Ergotamine, combined with caffeine (vasoconstriction), GI issues, teratogenesis, monitor V/S, separate ergot alkaloid from triptans by 24 hours

Preventive) Beta-blockers

Substance Use Disorders

Biologic response: higher dose for effect

Addiction: Overwhelming compulsion, despite health/social consequences

Prevention: Lowest dose, shortest duration

Substance Use Disorder: Self-administration, overwhelming desire to take a drug, can’t stop

Psychological Dependence: Overwhelming desire, craving; relapse (Opioids, drugs for insomnia, anti-anxiety drugs)

Physical Dependence: Opioids, alcohol, sedatives, nicotine; nervous system adapts to repeated substance use; uncomfortable withdrawal symptoms

Substance Use Disorders: Drug Classifications

Psychedelics/Hallucinogens: Schedule I drugs, LSD: fungus on rye

Dissociative Drugs: Ketamine, Sedation, Depression treatment, Facilitated assault

CNS Depressants

Benzodiazepines: Anti-anxiety (GABA), Reversal agent: Flumazenil, Withdrawal: insomnia, seizures, nausea, sensitivity to light and sound, headache, twitches

Alcohol: CNS depressant, food slows absorption, hepatitis, Treatment: benzodiazepines, Disulfiram (no alcohol)

Opioids: Intense withdrawal symptoms, not life-threatening, High psychological dependence, dilated pupils, HTN

Cannabinoids: THC – Marijuana, Bloodshot eyes, Weight gain, N/V, Withdrawal: irritability, chills, weight loss, tremors

Psychostimulants:

Amphetamines/Methylphenidate: Increase dopamine, Methylphenidate; Cocaine (vasoconstriction), Withdrawal: depression and anxiety, fatigue, and hunger

Nicotine: Withdrawal: irritability, anxiety, restlessness, headache, insomnia, inability to concentrate

Nurses' Roles: Medical history, nonjudgmental but firm, therapeutic relationship, involve family members, with IV: HIV, Hepatitis, TB, identify triggers and build supportive social connections

Antibiotic Therapy

Cell Wall: Penicillins, Cephalosporins, Carbapenems (Beta-lactams have a beta-lactam ring; interfere with bacterial cell-wall construction). Vancomycin - most widely U.S. hospitals

Protein Synthesis: Tetracyclines, Macrolides, Clindamycin, Linezolid

Bactericidal Protein Synthesis: Aminoglycosides

Antimetabolites(folic acid): Sulfonamides/Trimethoprim

Miscellaneous Antibacterial(DNA or RNA): Fluoroquinolones

Antimicrobial, Antibacterial, Antibiotic

Antimicrobial Kills/slows micros → Antibacterial – an antimicrobial that targets bacteria → Antibiotic – Bacterial infections, killing or inhibiting growth

Not all antibacterial agents are antibiotics.

Antibacterials/Antibiotics Overview

Identify organism (culture) → Drug sensitivity (which drug) → Consider patient factors (pregnancy, age, allergies)

Indications: Bacterial infections, empiric treatment (fever in a high-risk immunocompromised patient), prevent bacterial infections in selected situations (surgery, endocarditis, UTI/STI)

Nursing education: Only treat bacterial infections, not viruses, fungal infections, colds, or the flu. Side effects: N/V, diarrhea, yeast infections, allergic reaction. All antibacterials can cause superinfections.

Narrow-Spectrum Antimicrobials: Target only a few; less disruptive; less risk of drug resistance. and superinfections (favor these)

Broad-Spectrum Antimicrobials: Target a wide variety; disrupt normal flora, increase superinfections, and promote resistance (only in emergencies).

Drug Resistance: Decreased Drug Concentration → Target Alteration: Bacteria change the antibiotic’s binding site → Alternative Enzymes → Inactivating Enzymes: Bacteria produce enzymes that destroy or inactivate the antibiotic → antibiotic can’t kill bacteria that are resistant to proliferation

Superinfection: A NEW infection during the course of treatment for a primary infection (C. diff, Candidiasis, MRSA, VRE)

Selective Toxicity: Harms microbes without harming host cells.

Gram +: Thick cell wall, no outer membrane; easier for antibiotics to penetrate

Gram -: Thin cell wall, extra outer membrane; additional barrier

Bacterial Cell Wall Synthesis: Penicillins, Cephalosporins, Carbapenems (beta-lactam ring), Vancomycin - most widely used in U.S. hospitals

Penicillins: Penicillin G, amoxicillin, clavulanate; pneumonia, respiratory infections, UTIs, STIs, otitis media. Prophylaxis: use in susceptible patients; AEs: allergic reactions, superinfections, SJS/TEN, neurotoxicity, C. diff. Cautions: Hypersensitivity (1% cross-sensitivity to cephalosporins), renal impairment, asthma, bleeding, GI, pregnancy/lactation. Interactions: Tetracyclines decrease effectiveness, aminoglycosides(give penicillin first), anticoagulants/warfarin.

Cephalosporins: Cephalexin (Keflex); “ceph-” or “cef-.”→ Respiratory infections, STIs, otitis media, sinusitis, and bone and joint infections. AEs: Hypersensitivity, cross-sensitivity. Precautions: Renal impairment (Nephrotoxicity); (urine above 30 mL/hour; creatinine, BUN, GFR); bleeding or alcohol. IM injection may be painful. The newer generations of drugs work against MORE Gram-negative bacteria

Carbapenems/Imipenem: broad-spectrum, meningitis, unknown. Not effective against MRSA. Seizures due to reduced valproate levels. Cilastatin protects imipenem from being destroyed by the dipeptidase in the kidneys

Glycopeptide/Vancomycin (not a beta-lactam): Serious bacterial infections, MRSA, S. epidermidis, C. difficile, or penicillin allergies. Systemic: give IV (parenterally); C. diff: give PO; reduce the dose for kidney impairment. AEs: Nephrotoxicity, ototoxicity, flushing syndrome (Rash, pruritus, urticaria). Precautions: renal dysfunction, hearing loss, older adults, and neonates.

Bacteriostatic Protein Synthesis: Tetracyclines, Macrolides, Clindamycin, Linezolid

Bactericidal Protein Synthesis: Aminoglycosides

Tetracyclines: ”-cycline” Rickettsial diseases, chlamydia, Mycoplasma pneumoniae infections, Lyme disease, anthrax, acne, peptic ulcer disease, and periodontal. AEs: GI irritation, bone growth and teeth discoloration in pregnancy or in children <8 years old, superinfections, photosensitivity, hepatotoxicity, nephrotoxicity. Interactions: Empty stomach with water (throat irritation). Avoid dairy products, calcium, iron, antacids, and laxatives. Digoxin toxicity

Macrolides/Erythromycin. Pertussis (whooping cough), diphtheria, Chlamydia - combine with tetracyclines as indicated. Alternative to penicillin G. AE’s: QT prolongation, cardiac death, hepatotoxicity. Interactions: CYP450 inhibitors (liver), calcium channel blockers, nefazodone, Class I and III antiarrhythmic drugs, digoxin, warfarin.

Clindamycin. Risk of C. difficile infection; anaerobic bacterial infections; does not cross BBB; adjuvant therapy for severe streptococcal infections. AE: watery diarrhea, 10–20 episodes/day, pain, fever, leukocytosis; enhanced neuromuscular-blocking effects, such as with succinylcholine; ventilatory support available

Linezolid. Vancomycin-resistant enterococci (VRE), (MRSA), pneumonia, Staphylococcus epidermidis, severe Gram-positive infections. Not effective against Gram-negative bacteria. AE: myelosuppression/neuropathy. Tyramine-containing foods (Processed meats, aged cheeses, soy) → HTN; SSRIs serotonin syndrome

Aminoglycosides/Gentamicin/Tobramycin. Kills. Gram-negative infections, sepsis, UTIs, gonorrhea, and meningitis in infants. Combined with vancomycin, cephalosporins, or penicillins → Gram-positive cocci. AEs: Nephrotoxicity kidney damage and ototoxicity. If Oliguria or anuria develops, stop. Interactions: Penicillins give first, cephalosporins, vancomycin, ototoxic drugs, nephrotoxic drugs, and skeletal muscle relaxants. Caution: renal/hearing impairment, myasthenia gravis, neuromuscular blocking agents. Monitor BUN and creatinine

Antimetabolites(folic acid): Sulfonamides, Trimethoprim

DNA: Fluoroquinolones

Sulfonamides & Trimethoprim (hyperkalemia): chronic UTIs, STIs, burn care, and ophthalmic use. AE's: photosensitivity, SJS, hemolytic anemia, kernicterus (brain damage in newborns due to jaundice [Increased bilirubin), renal damage, hemolytic anemia in patients with G6PD deficiency, neurotoxicity. Interactions: Warfarin, phenytoin, and sulfonylureas. Precautions: pregnancy, breastfeeding, infants younger than 2 months of age. Renal impairment, folate deficiency, megaloblastic anemia; drink water

Fluoroquinolones/Ciprofloxacin: DNA. Bone, skin, joint, traveler’s diarrhea; multidrug-resistant TB. Drug of choice for anthrax; alternate parenteral antibiotics. AE’s: Restlessness, confusion, candidiasis, C. diff, tendon rupture (discontinue drug with tendon pain), phototoxicity. Older adults: confusion,psychosis. Milk, calcium, iron, zinc supplements; aluminum- magnesium-containing antacids; sucralfate reduce absorption. Warfarin. Precautions: Myasthenia gravis, people in the sun, older adults, renal impairment, glucocorticoids, transplants, <18 years old.

Photosensitivity (FST), Neurotoxicity (VASTC), C. diff risk (PCFT)

Photosensitivity: Fluoroquinolones, Sulfonamides, Tetracyclines

Neurotoxicity: Vancomycin, Aminoglycosides, Sulfonamides, Tetracyclines, Cephalosporins

C. diff: Penicillins, Clindamycin, Fluoroquinolones, Tetracyclines

CYP450 Inducers/Inhibitors

Inducers - CRAP GPS Carbamazepine Rifampin Alcohol (Chronic) Phenytoin Griseofulvin Phenobarbital Sulphonylurea

Inhibitors - CRACK AMIGOS Cimetidine Ritonavir Aminodarone Ciprofloxacin Ketoconazole Alcohol (Acute) Macrolides Isoniazide Grapefruit Juice Omeprazole Sulfonamides

Neurotransmitters

BBB: Entry of drugs into the brain; lipid-soluble; not fully developed at birth

Peripheral Nervous System: Acetylcholine, Norepinephrine, Epinephrine

Central:

Serotonin (Mom): Stabilizing. Side effects: GI disturbances, serotonin syndrome (fatal), mental status, tremors, tachycardia, and fever.

Norepinephrine (Dad): Excitatory (gets messages moving). Side effects: Hyperhidrosis (excessive sweating), hypertension, and dizziness. Taper

Dopamine (Funcle): Excitatory + Focus, pleasure, reinforcing behaviors, converts into norepinephrine. Effects: Motor coordination, sexual/addictive. Movement, Memory, Motivation, Mood.

GABA (Grandma): Gamma-aminobutyric acid, inhibits the nervous system.

Glutamate (Cowboy): Excitatory, memory → excitotoxicity/neuronal death.

Acetylcholine (ACh): Muscarinic receptors: Parasympathetic nervous system. Binds to nicotinic receptors to stimulate skeletal muscle contraction. Stimulates the adrenal medulla to release adrenaline (epinephrine) and norepinephrine.

Status Epilepticus - Benzodiazepine: first-line treatment, ventilation, glucose

Baclofen: hyper-spasticity, spasms related to MS/spinal cord injuries, CNS depressant, drowsiness, taper, hallucinations, paranoia, intrathecal seizures, rhabdomyolysis, death, urinary retention

Cyclobenzaprine (Fexmid, Flexeril): Local muscle relaxant for spasms; drowsiness, dizziness, fatigue, sympathetic response, dry mouth, blurred vision, photophobia, urinary retention, constipation. Contraindicated with MAO inhibitors

Parkinson Disease, Levodopa/Carbidopa

Slowly progressing neurodegenerative disorder. Too little dopamine and too much ACh; relief for ADLs; dopamine can’t cross the BBB; Levodopa can (effective)

Levodopa/Carbidopa (Sinemet): Levodopa → dopamine/AHc in the brain. Combined with carbidopa (does nothing on its own). Without Carbidopa, only 2% of levodopa is available in the brain. AEs: Nausea; too much dopamine: dyskinesias/ticks (LID); too little dopamine: freezing, bradykinesia (slowness), on-off phenomenon, sudden loss of effect, hypotension, and psychosis

First-generation antipsychotics (less effective)

Nonselective MAO inhibitors (HTN)

High-protein meals (reduce therapeutic effects).

Seizure Medications: Reduce seizures

Sodium

Oxcarbazepine (Trileptal) - Focal seizures, hyponatremia, hypothyroidism, dizziness, vision problems, blood dyscrasias, teratogenic, SJS & TEN

Carbamazepine (Tegretol) - Focal seizures, bipolar disorder, pain relief, serum drug levels, SJS/TEN; Asian descent increases risk, neural teratogen, avoid grapefruit juice (increases), hematologic toxicity (CBC), CYP inducers

Phenytoin (Dilantin) - Seizures except absence, (10-20 mcg/mL), SJS/TEN increase with Asian descent (HLA-B*1502), Teratogenic, monitor serum levels, gingival hyperplasia, purple glove syndrome. Many Drug interactions, CYP inducers

GABA

Valproate (Depakote) - Epilepsy, bipolar, migraine, teratogenic in first trimester, liver failure, pancreatitis, hyperammonemia, many drug interactions, other antiepileptic drugs, carbapenem antibiotics

Phenobarbital - Drowsiness, avoid CNS depressants (hyperactivity in children), long half-life 4 days, teratogenic, oldest antiseizure, lethargy, depression, learning impairment, taper or else → status epilepticus (5+ min), CYP inducer

Gabapentin (Neurontin) - Gaba/not known, epilepsy, adjunctive therapy of focal seizures, postherpetic neuralgia, 80% written for off-label. Somnolence/drowsiness, dizziness, rare drug interactions, abuse potential

Sodium + Calcium

Lamotrigine (Lamictal) - SJS/TEN (higher risk with Valproate), suicidality

Topiramate (Topamax) - Calms/GABA/Glutamate, seizures, migraine, eating disorders, weight loss, cause: metabolic acidosis, hypohidrosis, hyperthermia, suicidality

Unknown

Levetiracetam (Keppra) - Seizures, migraines, bipolar, neuropsychiatric symptoms (agitation, anxiety, depression, psychosis), does not impair speech or concentration, asthenia, few drug interactions (not metabolized by P450)

Trial period is over (drive), monitor plasma drug levels, taper, seizure chart, lower contraceptives, but seizures while pregnant are a risk

Urinary Anti-Infective: Nitrofurantoin (Macrobid)

Lower urinary tract infections, prophylaxis, and recurrent UTI’s

Discoloration of urine, pulmonary, hemolytic anemia (G6PD), peripheral neuropathy, hepatotoxicity (liver), birth defects (38-42 weeks), Antacids decrease effect, high concentrations: -cidal

Antitubercular: Isoniazid + Rifampin for all types of TB & Hansens/Leporsy

Isoniazid: pyridoxine B6 to prevent peripheral neuropathy (blocks cell wall synthesis); CYP450 inhibitor

Rifampin: turns urine/body fluids orange-red (blocks RNA synthesis); CYP450 Inducer (only inducer), oral birth control double up, teratogenic, warfarin

AEs: Hepatotoxicity (liver, no alcohol, Jaundice, peripheral neuropathy, psychological effects, cutaneous and flu symptoms)

Antifungal - Amphotericin B, Nystatin, Itraconazole & Ketoconazole

Amphotericin B - Systemic mycoses infections; ergosterol; Hypokalemia + renal (kidney) impairment; avoid nephrotoxic drugs (NSAIDS, aminoglycosides, vancomycin); Amphotericin B + Flucytosine can reduce the risk of toxicity.

Nystatin - Orally, vaginal, topical. Superficial fungal infections: candidiasis, skin, mouth, esophagus, and vagina

Itraconazole (systemic and superficial; food and acidic beverages increase absorption, caution with heart, ventricular, pulmonary, or liver disease) & Ketoconazole (no systemic infections), 14α-demethylase → ergosterol; dermatophyte/tinea (ringworm, athlete’s foot), candidiasis. AEs: Cardiac suppression, liver, and teratogenic. Decrease the dose of simvastatin. CYP inhibitor

Herpes, HSV-1+2, Varicella Zoster Virus - Acyclovir (Zovirax)

Prevents viral DNA replication in mucocutaneous tissue; cytomegalovirus is resistant; stay hydrated; precaution with seizure and obesity.

Phlebitis, burn, sting, nephrotoxicity, neurologic (kidney/renal) toxicity, GI, vertigo

Genital Herpes: Does not eliminate the virus; it only decreases symptoms and promotes healing (no cure)

Oral therapy for varicella-zoster infections → 24 hours after rash onset in immunocompromised. IV therapy can cause reversible nephrotoxicity.

Antivirals, Neuraminidase Inhibitors - Oseltamivir (Tamiflu)

Prophylaxis/treatment of flu in those> 1 year old and pregnant: begin 48 hours before exposure; take for 10 days. AEs: Headache, N/V

D/C: 2 days before vaccine, 2 weeks after vaccine. Not a replacement for vaccination

HIV Nucleoside Reverse Transcriptase Inhibitors - Abacavir (Ziagen)

HIV Protease Inhibitors - Ritonavir (Norvir)

HIV retrovirus (RNA genetic material) initial phase: flu-like. Middle phase: 10 years, asymptomatic, CD4 T-cells decline. Late phase/AIDS: CD4 T-cell count <200 cells/mL

Abacavir - Add another antiretroviral drug to avoid resistance, hypersensitivity (HLA-B*5701), acidosis, hepatomegaly (large fatty liver), alcohol, lipodystrophy, Cushing, look up drug interactions

Ritonavir – Low-dose booster, HIV protease & cancer. CYP3A4 inhibitor/inducer. AEs: Metallic taste, GI, hyperglycemia, diabetes, lipodystrophy. -Statins increase risk of toxicity & muscle damage, hyperlipidemia, PR/QT interval prolongation, pancreatitis

Antiprotozoal Drugs - Metronidazole

Narrow-spectrum anaerobic protozoal antibacterial; inhibits DNA/RNA synthesis = death. Bacterial vaginosis. Avoid all alcohol products or disulfiram reaction (shaving cream, cough syrup). AEs: metallic taste/black hairy tongue, stomatitis, dark urine, insomnia, hypersensitivity, SJS, aseptic meningitis, peripheral neuropathy. Contraindications: warfarin, CYP450 inhibitors (-azole)

Antimalarial - Atovaquone/Proguanil

Travel prophylaxis: 1-2 days before travel, during, and 7 days post-trip

Exoerythrocytic (liver) phase = outside RBCs; harder to treat; erythrocytic (blood) phase = inside RBCs

Atovaquone – inhibits Plasmodium parasite DNA synthesis. Tetracycline and rifampin reduce it by 50%. GI upset, headache, fever, and insomnia.

Proguanil – Prevents folate-dependent DNA synthesis. Oral ulcers, GI upset, urticaria, scaling of the soles and palms.

Administer with food or a milk-like drink to reduce GI upset, Monitor AST and ALT.