Pharmacology: Cardiac, Pain, Antimicrobial, and Chemotherapy Agents

Vocabulary flashcards covering pharmacology lecture notes across cardiovascular agents, analgesics, antimicrobials, bone and gout medications, antifungals, antivirals, HIV therapies, and antineoplastic supportive care.

Captopril

(RMBR: ACE Inhibitor = -pril)

Action: ACE inhibitor that blocks the conversion of angiotensin I to angiotensin II, causing vasodilation, decreased aldosterone, and increased bradykinin levels.

Therapeutic uses: hypertension, heart failure, and diabetic nephropathy, myocardial infarction, prevention of MI, stroke, and death in patients at high cardiovascular risk.

Adverse effects: dry cough, hyperkalemia, first-dose hypotension, and angioedem, renal failure, fetal injury, neutropenia.

Drug Interactions: diuretics, antihypertensive agents drugs that raise potassium levels, salt substitutes, lithium, nonsteroidal anti-inflammatory drugs.

Losartan

(RMBR: ARBs = -tan)

Action: Angiotensin II Receptor Blocker (ARB) blocks angiotensin II from binding to its receptors, causes dilation of arterioles and veins, prevent angiotensin ll from inducing pathologic, reduce excretion of potassium, decrease release of aldosterone, increase renal excretion of sodium and water, do not inhibit kinase ll, do not increase levels of bradykinin.

Therapeutic uses: hypertension, heart failure, myocardial infarction, diabetic nephropathy, may prevent development of diabetic retinopathy, use in patients unable to tolerate ACE inhibitors

Adverse effects: Angioedema, fetal harm, renal failure, lower instance of cough

Drug Interactions: Antihypertensive agents

Aliskiren

Action: Direct renin inhibitor which binds tightly to renin and inhibits the conversion of angiotensinogen into angiotensin I.

Therapeutic Uses: Hypertension

Pharmacokinetics: Oral administration; high fat meals lower availability

Side Effects: angioedema, cough, GI effects, hyperkalemia, fetal injury & death

Drug interactions: atorvastatin and ketoconazole (will raise levels of aliskiren); furosemide levels will be lowered

Eplerenone

Action: selective blockage of aldosterone receptors, also a potassium-sparing diuretic

Therapeutic Uses: hypertension, heart failure

Pharmacokinetics: absorption is not affected by food

Adverse effects: hyperkalemia

Drug interactions: inhibitors of CYP3A4, drugs that raise potassium levels, use with caution when combined with lithium

Spironolactone

Aldosterone Antagonist and Potassium Sparing Diuretic

Action: blocks aldosterone receptors (aldosterone antagonist),binds with receptors for other steroid hormones, blocks aldosterone in the distal nephron, retention of potassium, increased excretion of sodium

Therapeutic uses: hypertension, heart failure, Primary hyperaldosteronism, Premenstrual syndrome, Polycystic ovary syndrome, Acne in young women

Adverse effects: hyperkalemia, gynecomastia, menstrual irregularities, impotence, hirsutism, deepening of the voice, benign and malignant tumors, endocrine effects

Diltiazem

Nondihydropyridine calcium channel blocker

Therapeutic uses: angina pectoris, Hypertension, Cardiac dysrhythmias(Atrial flutter, atrial fibrillation, paroxysmal tachycardia)

Pharmacokinetics: IV and Oral administration and Hepatic metabolism and excretion

Actions: Blocks calcium channels in the heart and blood vessels (like verapamil), Lowers blood pressure (Arteriolar dilation and Direct suppressant/reflex cardiac stimulation = Little net effect on the heart)

Adverse effects: Similar to verapamil (except for less constipation), Dizziness, Flushing, Headache, Edema of ankles and feet, Exacerbates bradycardia, sick sinus syndrome, heart failure, second- or third-degree heart block

Drug interactions: Digoxin and Beta-adrenergic blocking agents

Verapamil

Nondihydropyridine calcium channel blocker

Therapeutic uses: angina pectoris (vasospastic angina and angina of effort), essential hypertension (second line agent after thiazide diuretics), cardiac dysrhythmias (atrial flutter, atrial fibrillation, paroxysmal supraventricular tachycadia), migraine

Pharmacokinetics: IV and oral administration, hepatic metabolism and excretion

Adverse effects:

• Constipation (most common complaint)- due to blockade of calcium channels in smooth muscle of intestine, especially severe for older adults, can be decreased by increasing fiber and fluids

• Dizziness, facial flushing, headache, edema of ankles and feet, gingival hyperplasia, heart block

Drug Interactions: digoxin, beta-adrenergic blocking agents, grapefruit juice

Toxicity: severe hypotension, bradycardia and AV block, ventricular tachydysrhythmias, gastric lavage and activated charcoal

IV verapamil for dysrhythmias can cause severe cardiovascular effects

• monitor blood pressure and ECG, and keep resuscitation equipment close

Nifedipine

(RMBR: dihydropyridines= -pine)

Dihydropyridine calcium channel blocker

Therapeutic uses: Angina pectoris, Hypertension, Cannot be used to treat dysrhythmias

Pharmacokinetics: Oral administration, Metabolized by liver excreted by kidneys.

Immediate release (not sustained)- Has been associated with increased mortality in patients with MI and unstable angina, Other rapid-acting calcium channel blockers also associated, No cause-and-effect relationship established, Use with caution

Actions: Vasodilation by blocking calcium channels: Lowered blood pressure, Increased heart rate, Increased contractile force

Adverse effects:Flushing, Dizziness, Headache, Peripheral edema, Gingival hyperplasia, Chronic eczematous rash in older patients, Reflex tachycardia, Increases cardiac oxygen demand, Can increase pain in angina patients,

Can be combined with a beta blocker for prevention of reflex tachycardia- Note: Beta blockers decrease the adverse cardiac effects of nifedipine but can intensify the adverse cardiac effects of verapamil and diltiazem

Hydralazine

Direct-acting vasodilator

Therapeutic uses: Essential hypertension, Hypertensive crisis, Heart failure

Actions: Selective dilation of arterioles, Mechanism unknown, Postural hypotension minimal

Pharmacokinetics: Oral and IV administration, Oral onset 45 minutes, duration 6 hours, IV onset 10 minutes, duration 2-4 hours,Dosage is individualized due to acetylation

Adverse effects: Reflex tachycardia, Increased blood volume, Systemic lupus erythematosus–like syndrome, Headache, dizziness, weakness, and fatigue

Drug interactions: Other antihypertensive agents, Avoid excessive hypotension, Combined with beta blocker to protect against reflex tachycardia and with diuretics to prevent sodium and water retention and expansion of blood volume

Minoxidil

Vasodilator

Therapeutic Uses: Used for severe hypertension unresponsive to safer drugs, Also known as Rogaine for hair growth

Action: Selective dilation of arterioles, More intense dilation than hydralazine, but causes more severe adverse reactions

Adverse effects: Reflex tachycardia, Sodium and water retention, Hypertrichosis, Pericardial effusion, Other

Sodium Nitroprusside

Vasodilator

Therapeutic Uses: Used for hypertensive emergencies

Action: Fastest-acting antihypertensive agent, Causes venous and arteriolar dilation

Pharmacokinetics: Administration: IV infusion, Onset: Immediate (BP returns to pretreatment level in minutes when stopped)

Adverse effects: Excessive hypotension, Cyanide poisoning, Thiocyanate toxicity,Fluid retention

Furosemide (Lasix)

Ethacrynic acid, bumetanide, torsemide

Loop Diuretic

Pulmonary edema, Edematous states, Hypertension

Mechanism of action: Acts on ascending loop of Henle to block reabsorption

Pharmacokinetics: Oral and IV, Rapid onset (PO 60 minutes; IV 5 minutes)

Drug interactions: Digoxin, Ototoxic drugs (e.g., gentamicin), Potassium-sparing diuretics, Lithium, Antihypertensive agents, Nonsteroidal anti-inflammatory drugs

Adverse effects: Hyponatremia, hypochloremia, and dehydration, Hypotension (Loss of volume and Relaxation of venous smooth muscle),Hypokalemia, Ototoxicity, Hyperglycemia, Hyperuricemia, Use in pregnancy, Impact on lipids, calcium, and magnesium

Hydrochlorothiazide (HydroDIURIL)

Chlorothiazide

Thiazide Diuretic

Therapeutic uses: Essential hypertension, Edema, Diabetes insipidus

Action:Early segment distal convoluted tubule

Pharmacokinetics: Oral and IV, Peaks in 4 to 6 hours

Adverse effects: Hyponatremia, hypochloremia, and dehydration, Hypokalemia, Use in pregnancy and lactation, Hyperglycemia, Hyperuricemia, Impact on lipids, calcium, and magnesium

Drug interactions: Digoxin, Augments effects of hypertensive medications, Can reduce renal excretion of lithium (leading to accumulation), NSAIDs may blunt diuretic effect, Can be combined with ototoxic agents without increased risk of hearing loss

Mannitol

Osmotic Diuretic

Therapeutic uses: Prophylaxis of renal failure, Reduction of intracranial pressure, Reduction of intraocular pressure

Action: Promotes diuresis by creating osmotic force within lumen of the nephron

Pharmacokinetics: Drug must be given parenterally.

Adverse effects: Edema, Headache, Nausea, Vomiting, Fluid and electrolyte imbalance

Sacubitril/Valsartan (Entresto)

Angiotensin receptor-neprilysin inhibitor (ARNI)

Action: Suppresses the negative effects of the RAAS system, Reduces hospitalizations, mortality, and risk of death from cardiovascular causes

Side effects: Angioedema, hyperkalemia, hypotension

Nitroglycerin

Vasodilator Organic Nitrates

Uses:stable angina, variant angina, hypertensive crisis 

Action: Vasodilation of veins at therapeutic doses, reduces preload and oxygen demand

Pharmacokinetics: Oral (sublingual), IV, topical, 5-7 minute half life

Tolerance:Can develop rapidly, Cross-tolerance to all other nitrates, To minimize use the lowest effective dose, Long-acting formulas: 8 drug-free hours per day

Adverse effects: headache, orthostatic hypotension, reflex tachycardia

Interactions: Hypotensive drugs, Beta blockers, verapamil, and diltiazem, Sildenafil [viagra], people with aortic stenosis

Considerations: discontinue gtt slowly

Education: Light sensitive container, Expiration date, Sit down when taking it, Hold under tongue    

Take 1 dose, wait 5 minutes if no symptom resolution. Call 911 and take 2nd dose. Take a second, wait 5 minutes if no symptom resolution. Take 3rd dose.

Digoxin (Lanoxin, Lanoxicaps, Digitek)

Cardiac glycoside positive inotropic agent

Action: Increases myocardial contractility, Increased cardiac output, Positive inotropic action on the heart, Increases force of ventricular contraction, Increases myocardial contractility

Benefits: Hemodynamic, Neurohormonal, Electrical

Pharmacokinetics: Oral, IV, Absorption is variable, Distributed widely and crosses placenta, Eliminated primarily by renal excretion, Half-life about 1.5 days

Adverse effects: Cardiac dysrhythmias

Conditions that increase the risk of dysrhythmias: Hypokalemia, Elevated digoxin level, Narrow therapeutic range, Heart disease

Toxicity: Halo around lights, Nausea, vomiting, diarrhea

Drug interactions: Diuretics, ACE inhibitors and ARBs, Sympathomimetics, Quinidine, Verapamil

Has very narrow therapeutic optimal level: 0.5-0.8 ng/mL

Quinidine

Class IA sodium channel blocker

Therapeutic uses: Used for supraventricular and ventricular dysrhythmias

Effects on the heart: Blocks sodium channels, Slows impulse conduction, Delays repolarization, Blocks vagal input to the heart

Effects on the ECG: Widens the QRS complex, Prolongs the QT interval

Pharmacokinetics: Oral

Adverse effects: Diarrhea, Cinchonism, Cardiotoxicity, Arterial embolism, Alpha-adrenergic blockade, resulting in hypotension, Hypersensitivity reactions

Drug interactions: Digoxin

Lidocaine (Xylocaine)

Class IB sodium channel blocker

Effects on the heart and ECG: Blocks cardiac sodium channels, Reduces automaticity in the ventricles and His-Purkinje system, Accelerates repolarization

Adverse effects: CNS effects (Occur at high therapeutic doses, Reduce infusion rate), Drowsiness, Confusion, Paresthesias

Amiodarone (Cordarone, Pacerone)

Class III potassium channel blocker

Therapeutic uses: For life-threatening ventricular dysrhythmias only, Recurrent ventricular fibrillation, Recurrent hemodynamically unstable ventricular tachycardia

Effects on the heart and ECG: Reduced automaticity in the SA node, Reduced contractility, Reduced conduction velocity, QRS widening, Prolongation of the PR and QT intervals

Pharmacokinetics: Oral, IV

Adverse effects: Pulmonary toxicity, Cardiotoxicity, Liver toxicity, Pregnancy and breastfeeding, Corneal microdeposits, Optic neuropathy

Atorvastatin, Lovastatin, Simvastatin

HMG-CoA reductase inhibitor

Uses: Hypercholesterolemia, Primary and secondary prevention of CV events, Primary prevention with people with normal LDL, Post MI therapy, Diabetes

Action & Benefits: Reduction of LDL cholesterol, Elevation of HDL cholesterol, Reduction of triglyceride levels,Nonlipid beneficial cardiovascular actions, Increased bone formation

Pharmacokinetics: Oral, Metabolized and excreted by liver, Administer in evening

Adverse effects: headache, rash, memory loss, or GI disturbances, cataracts, Myopathy and Rhabdomyolysis, hepatotoxicity

Interactions: Other lipid lowering agents, Drugs that inhibit CYP3A4

Colesevelam

Bile acid sequestrant

Uses: adjunct therapy to diet and exercise for people with primary hypercholesterolemia, T2DM

Action: Reduces LDL cholesterol, Increases VLDL levels in some patients, Increases LDL receptors on hepatocytes, Prevents reabsorption of bile acids

Adverse effects: constipation, Hypoglycemia

Interactions: thiazide diuretics, digoxin, warfarin, and some antibiotics

Ezetimibe

Cholesterol absorption inhibitor

Therapeutic uses: Reduces total cholesterol, LDL cholesterol, and apolipoprotein B, Approved for monotherapy and combined use with statins

Action: Inhibits cholesterol absorption

Pharmacokinetics: oral, metabolized and excreted by liver

Adverse effects: Myopathy, Rhabdomyolysis, Hepatitis, Pancreatitis, Thrombocytopenia

Drug interactions: Statins, Fibrates, Bile-acid sequestrants, Cyclosporine

Gemfibrozil

Fibric acid Derivative

Therapeutic uses: Reduces high levels of plasma triglycerides (VLDLs), Treatment reserved for patients who have not responded to diet modification, Less effective than statins in reducing LDL, Can raise HDL (not approved for this use)

Action: Decreases plasma TG content, Lowers VLDL levels, Can raise HDL cholesterol, Appears to interact with a specific receptor subtype (PPAR alpha)

Adverse Effects: Rashes, Gastrointestinal disturbances, Gallstones, Myopathy, Liver injury (hepatotoxic)

Drug interactions: Displace warfarin from plasma albumin, Measure international normalized ratio (INR) frequently

Heparin

Unfractionated anticoagulant

Uses: Preferred anticoagulant during pregnancy and when rapid anticoagulation is required, Pulmonary embolism (PE), Stroke evolving, Massive deep vein thrombosis (DVT), Open heart surgery, Renal dialysis, Low-dose therapy postoperatively, Disseminated intravascular coagulation (DIC), Adjunct to thrombolytic therapy

Action: Enhances antithrombin, Rapid-acting anticoagulant

Pharmacokinetics: Administered by injection only (IV: Continuous and intermittent and Deep subcutaneous (subQ)

Adverse effects: Hemorrhage, Heparin-induced thrombocytopenia (HIT), Hypersensitivity reactions

Contraindicated: Thrombocytopenia, Uncontrollable bleeding, During and immediately after surgery of the eye, brain, or spinal cord

Monitoring: partial thromboplastin time (PTT) or anti-Xa heparin assay, Nurse driven protocols, 2 RN double check, stopping and restarting for labs and procedures 

Antidote for overdose: Protamine sulfate

Enoxaparin (Lovenox)

Low-molecular-weight heparin (LMWH)

Therapeutic uses: Prevention of DVT after surgery, Treatment of established DVT, Prevention of ischemic complications

Action: composed of molecules that are shorter than those found in unfractionated heparin

Pharmacokinetics: SubQ- lower abdomen is preferred, dose based on body weight, does not require monitoring

Adverse effects and interactions: Bleeding (but less than with unfractionated heparin), Bruising at site of injection, Immune-mediated thrombocytopenia, Severe neurologic injury for patients undergoing spinal puncture or spinal epidural anesthesia

For patients with severe renal impairment, dosage should be reduced

Warfarin (Coumadin)

Anticoagulant

Therapeutic uses: Not useful in emergencies, Long-term prophylaxis of thrombosis

Action: decreasing production of four clotting factors, namely, factors VII, IX, X, and prothrombin

Pharmacokinetics: Oral, Half life of 6.5 hours to 2.5 days, Monitor with INR, Usually given at 4pm

Considerations: heparin to warfarin bridge, stopping before surgery, patient education  

Adverse effects: Hemorrhage (vitamin K for toxicity), Fetal hemorrhage and teratogenesis from use during pregnancy, Use during lactation, Other adverse effects

Interactions: Drugs that increase anticoagulant effects, Drugs that promote bleeding, Drugs that decrease anticoagulant effects, Dietary vitamin K (leafy greens)

Dabigatran etexilate (Pradaxa)

Direct thrombin inhibitor

Therapeutic uses: Atrial fibrillation, Knee or hip replacement

Pharmacokinetics: Oral prodrug that undergoes conversion to dabigatran, renal excretion 13 hour half life

Adverse Effects: Bleeding, GI disturbances

Interactions: Combined use with a P-glycoprotein inhibitor (e.g., ketoconazole, amiodarone, verapamil, quinidine) could cause bleeding from excessive dabigatran levels

Aspirin (Antiplatelet)

Antiplatelet, NSAID

Therapeutic uses: Ischemic stroke, Transient ischemic attack (TIA), Chronic stable angina, Unstable angina, Coronary stenting, Acute MI, Previous MI, Primary prevention of MI

Action: suppresses platelet aggregation by causing irreversible inhibition of cyclooxygenase

Pharmacokinetics: Oral, Daily dosing 81mg, Emergency dosing: 325mg

Adverse effects: Bleeding, GI bleeding and hemorrhagic stroke, Enteric-coated tablets may not reduce the risk of GI bleeding

Clopidogrel (Plavix)

Antiplatelet agent

Therapeutic uses: Block P2Y₁₂ ADP receptors on the platelet surface, preventing ADP-stimulated aggregation, Prevents blockage of coronary artery stents.

Reduces thrombotic events in patients with acute coronary syndromes

• Prevents stenosis of coronary stents; also for secondary prevention of MI, ischemic stroke, and other vascular events

Adverse effects similar to those of aspirin

Use with caution in combination with other drugs that promote bleeding

Alteplase

Tissue plasminogen activator (tPA) thrombolytic

Therapeutic uses: Myocardial infarction, Ischemic stroke, Massive pulmonary emboli

Action: Binds with plasminogen to form an active complex, Alteplase-plasminogen complex then catalyzes the conversion of other plasminogen molecules into plasmin, an enzyme that digests the fibrin meshwork of clots

Adverse effects: Bleeding, Fever

Advantages: Does not cause allergic reactions, Does not induce hypotension

Morphine

Pure Opioid Agonists

Source: Seedpod of the poppy plant

Actions: Pain relief, Drowsiness, Mental clouding, Anxiety reduction, Sense of well-being

Therapeutic uses: Relieves pain without affecting other senses (eg, sight, touch, smell, and hearing), No loss of consciousness, Relieve pain by mimicking the actions of endogenous opioid peptides, primarily at muwh receptors

Administration: Oral, rectal, Intramuscular and subcutaneous, Intravenous, Epidural and intrathecal

General Guidelines: Individualized doses, Respiratory rate, blood pressure and pulse rate

Adverse Effects:

1) Respiratory Depression

• Infants and the elderly are especially sensitive

• Onset:

  • Intravenous, 7 minutes; intramuscular, 30 minutes; subcutaneous, up to 90 minutes; may persist 4 to 5 hours

  • Spinal injection: Response may be delayed by hours

• Tolerance to respiratory depression can develop

• Increased depression with concurrent use of other drugs that have CNS depressant actions (eg, alcohol, barbiturates, and benzodiazepines)

• Can compromise patients with impaired pulmonary function, Asthma, emphysema, kyphoscoliosis, chronic cor pulmonale, and extreme obesity

2) Neurotoxicity

• Delirium, agitation, myoclonus, hyperalgesia, and other symptoms

• Risk factors include renal impairment, pre-existing cognitive impairment, and prolonged high-dose opioid use

• Management: Hydration and dose reduction

3) Sedation

• Drowsiness and some mental clouding

• Avoid hazardous activities

• Sedation can be minimized:

  • Take smaller doses more often

  • Use opioids that have short half-lives

  • Give small doses of a CNS stimulant (eg, methylphenidate or dextroamphetamine)

  • Non-amphetamine stimulants such as modafinil [Provigil, Alertec] or armodafinil [Nuvigil] may also be tried

4) Constipation

• Cause: Suppressed propulsive intestinal contractions, intensified non propulsive contractions, increased tone of the anal sphincter, and inhibited secretion of fluids into the intestinal lumen

• Complications of constipation include fecal impaction, bowel perforation, rectal tearing, and hemorrhoids

• Treatment includes physical activity, increased intake of fiber and fluids, stimulant laxatives, stool softeners, and polyethylene glycol

5) Urinary retention and hesitancy

• Increases tone in the bladder sphincter

• Increases tone in the detrusor muscle, thereby elevating pressure within the bladder and causing a sense of urinary urgency

• May interfere with voiding by suppressing awareness of bladder stimuli

6) Orthostatic hypotension

• Morphine-like drugs lower blood pressure by blunting the baroreceptor reflex and by dilating peripheral arterioles and veins

• Patient teaching: Symptoms of hypotension (eg, lightheadedness and dizziness) and instructions to sit or lie down if they occur

• Hypotension can be minimized by moving slowly when changing from a supine or seated position to an upright position

7) Cough suppression

• Acts at opioid receptors in the medulla to suppress cough

• Suppression of spontaneous cough may lead to the accumulation of secretions in the airway

• Patients should be instructed to actively cough at regular intervals

• Codeine-based and hydrocodone-based cough remedies

8) Tolerance

• Increased doses needed to obtain the same response

• Develops with analgesia, euphoria, sedation, and respiratory depression

• Cross-tolerance to other opioid agonists

• No tolerance to miosis or constipation develops

9) Physical dependence

• Abstinence syndrome with abrupt discontinuation

• About 10 hours after last dose, the initial reaction occurs and includes yawning, rhinorrhea, and sweating

• Progresses to violent sneezing, weakness, nausea, vomiting, diarrhea, abdominal cramps, bone and muscle pain, muscle spasms, and kicking movements

• Lasts 7 to 10 days if untreated

• Withdrawal is unpleasant but not lethal, as it may be with CNS depressants

Toxicity

• Clinical manifestations: Classic triad

  • Coma, Respiratory depression, Pinpoint pupils

•Treatment: (Ventilatory support and Antagonist: Naloxone [Narcan])

Interactions

•CNS Depressants

•Anticholinergic Drugs

•Hypotensive Drugs

•Monoamine Oxidase Inhibitors

•Agonist-Antagonist Opioids

•Opioid Antagonists

Fentanyl

Potent pure opioid agonist

100 times the potency of morphine

Formulations given via three routes: Parenteral by Surgical anesthesia, Transdermal [Duragesic] by Patch (Heat acceleration) or Iontophoretic system (Needle-free), Transmucosal

Buprenorphine

Agonist-Antagonist Opioid

•7-day patch: Butrans

•Sublingual film: Suboxone

Naloxone (Narcan)

Opioid antagonist

Therapeutic uses: Reversal of opioid overdose, Reversal of postoperative opioid effects, Reversal of neonatal respiratory depression

Action & Effects: Competitive antagonist at opioid receptors, Blocks opioid actions

Pharmacokinetics: IV, IM, subQ, Intranasal, Immediate effects that persist for one hour, Repeat dose every 2-3 minutes

Methylnaltrexone

Peripherally acting opioid antagonist specifically designated for treating opioid-induced constipation.

Ibuprofen

Nonaspirin First-Generation NSAID

Inhibits cyclooxygenase and has anti-inflammatory, analgesic, and antipyretic actions

Indications: Fever, mild to moderate pain, arthritis

Generally well tolerated

Low incidence of adverse effects

SAFETY ALERT: All first-generation NSAIDs are associated with an increased risk of GI bleeding that can lead to hospitalization or death

Celecoxib

Second-generation selective COX-2 inhibitor

Reduces pain, fever, and suppresses inflammation, protects against colorectal cancer

•Second-generation COX-2 inhibitor: Fewer adverse effects than first-generation drugs

•Because of cardiovascular risks, last-choice drug for long-term management of pain. Increased risk of MI or stroke.

Adverse effects: Dyspepsia, Abdominal pain, Renal impairment, Sulfonamide allergy, Cardiovascular impact
(stroke, MI, and other serious events)

Acetaminophen

Therapeutic uses: Analgesic, antipyretic, Does not have any anti-inflammatory or antirheumatic actions

Action: Inhibits prostaglandin synthesis in central nervous system

Adverse effects: Very few at normal doses, Rarely: Stevens-Johnson syndrome (SJS), and toxic epidermal necrolysis (TEN), Hepatotoxicity

Overdose: Hepatic necrosis

•Signs and symptoms of hepatic failure, coma, death

•Early symptoms: Nausea and vomiting, diarrhea, sweating, abdominal pain

•Treatment for overdose: Acetylcysteine (Mucomyst)

Penicillin G (Benzylpenicillin)

Therapeutic uses: streptococcus species, Neisseria species, many anaerobes, spirochetes, others

Action: Bactericidal to numerous gram-positive and some gram-negative organisms

Pharmacokinetics: IM and IV administration, Minimal metabolism and excreted by kidneys  

Adverse effects:Least toxic of all antibiotics, Penicillins are the most common cause of drug allergy

Penicillin Allergy Types:

○Immediate (reaction in 2 to 30 minutes)

○Accelerated (reaction in 1 to 72 hours)

○Delayed (reaction takes days or weeks to develop)

Anaphylaxis: Laryngeal edema, Bronchoconstriction, Severe hypotension

Treatment: Epinephrine, Respiratory support, Prevention: Skin testing

Carbapenems: Imipenem (Primaxin)

Action: has an extremely broad antimicrobial spectrum, active against most bacterial pathogens (including organisms resistant to other antibiotics), highly active against gram-positive cocci and most gram-negative cocci and bacilli, use for treating patients with mixed infections in which anaerobes, S. aureus, and gram-negative bacilli, binds to two PBPs (PBP1 and PBP2), causing weakening of the bacterial cell wall with subsequent cell lysis and death, most effective beta-lactam antibiotic for use against anaerobic bacteria

Pharmacokinetics: not absorbed from the GI tract and hence must be given IV, penetrates the meninges to produce therapeutic concentrations in the CSF, renal excretion, 1 hour half life

Adverse effects: nausea, vomiting, diarrhea, headache, superinfections, seizures (rare), hypersensitivity reactions, 1% incidence of cross-sensitivity with penicillins

Interactions: Imipenem can reduce blood levels of valproate, causing breakthrough seizures

Vancomycin

Action: Inhibits cell wall synthesis by by binding to molecules that serve as precursors for cell wall biosynthesis.

Uses: Severe infections only, active only against gram-positive bacteria, MRSA, Staphylococcus epidermidis, Clostridium difficile

Pharmacokinetics: Oral and Intravenous administration, Vanco trough, Eliminated unchanged by kidneys, doses should be reduced  for renal impairment

Adverse effects: Renal failure, Ototoxicity (reversible or permanent), “Red man” syndrome, Thrombophlebitis (common), Thrombocytopenia (rare), Allergy

Interactions: Make sure to check IV compatibility!

Erythromycin, Clarithromycin, Azithromycin

Macrolides

Broad-spectrum antibiotics that inhibit bacterial protein synthesis.

They are called macrolides because they are big.

Erythromycin is the oldest member of the family.

The newer macrolides, azithromycin and clarithromycin, are derivatives of erythromycin

Clindamycin

Action: Bacteriostatic inhibitor of protein synthesis, Can promote severe Clostridium difficile–associated diarrhea (CDAD) (can be fatal), Active against most anaerobic bacteria (gram positive and gram negative)

Uses: Indicated only for certain anaerobic infections outside the central nervous system (CNS), Used as an alternative to penicillin

Pharmacokinetics: Oral,topical,IM, IV, Metabolized by liver, excreted in urine
and bile

Adverse effects:C. Diff, Diarrhea, Hepatic toxicity, Blood dyscrasias, Hypersensitivity reactions

Linezolid

Action:Bacteriostatic inhibitor of protein synthesis

Uses:Active against multidrug-resistant, gram-positive pathogens (eg, vancomycin-resistant enterococci [VRE], methicillin-resistant Staphylococcus aureus [MRSA])

Pharmacokinetics: Oral and IV, Hepatic metabolism, real excretion

Side Effects: Diarrhea, Nausea and vomiting, Headache, myelosuppression

Gentamicin, Tobramycin, Amikacin

Aminoglycosides

Action: disrupt bacterial protein synthesis, Bactericidal

Uses: infections due to aerobic gram-negative bacilli, Prophylactically for elective colorectal surgery, Conjunctivitis

Pharmacokinetics: Oral, IV, IM, topical, Not metabolized, eliminated by kidneys

Adverse effects: Ototoxicity, Nephrotoxicity, Inhibit neuromuscular transmission

Beneficial drug interactions: Penicillins, Cephalosporins and Vancomycin

Adverse drug interactions: Ototoxic drugs, Nephrotoxic drugs, Skeletal muscle relaxants

Trimethoprim/Sulfamethoxazole

Combination antibiotic

Uses: UTI, otitis media, bronchitis, shigellosis, pneumonia caused by Pneumocystis jiroveci, Pneumocystis pneumonia, and GI infection

Action: Inhibits sequential steps in bacterial folic acid synthesis, making it much more powerful than TMP or SMZ alone

Pharmacokinetics: Oral and IV, Plasma drug levels, Excreted primarily by kidneys

Adverse effects: Gastrointestinal, Rash, Hyperkalemia, Hypersensitivity reactions (Stevens-Johnson syndrome), Blood dyscrasias

Ciprofloxacin

Fluoroquinolone antibiotic

Action: Broad-spectrum antibiotic (gram-negative and some gram-positive organisms), Inhibits bacterial DNA gyrase and
topoisomerase II

Uses: Drug of choice for anthrax, Infections: Respiratory, urinary tract (UTI), GI, bones, joints, skin, and soft tissue

Pharmacokinetics: Oral and IV, Hepatic metabolism, renal excretion

Adverse effects: GI: Nausea/vomiting, diarrhea, abdominal pain, Central nervous system (CNS): Dizziness, headache, restlessness, confusion, rarely seizures, Tendon rupture, Phototoxicity, Candida infections: Pharynx and vagina, Increased risk of Clostridium difficile infection (CDI)

Absorption reduced by: Aluminum antacids, Magnesium antacids, Iron salts, Zinc salts, Sucralfate, Milk and dairy products

Metronidazole

Action: Bactericidal, lethal to anaerobic organisms only

Uses: Protozoal infections, Infections caused by obligate anaerobes, Helicobacter pylori

Pharmacokinetics: Oral and IV

Adverse effects: Neurotoxicity, Allergy, Superinfections

Daptomycin

Cyclic lipopeptide IV antibiotic

Uses: Bloodstream infection with S. aureus, and complicated skin and skin structure infections caused by susceptible strains of gram-positive bacteria

Action: Kills virtually all gram-positive bacteria, including methicillin-resistant S. aureus (MRSA)

Pharmacokinetics: Given only once daily IV: No laboratory work needed

Adverse effects: Possible muscle injury

No significant drug interactions

Colchicine

Antigout anti-inflammatory drug

Anti-inflammatory agent: No longer the first-line drug, Now reserved for patients who are unresponsive to or intolerant of safer agents, Not effective against other anti-inflammatory disorders

Uses: Treats acute gouty attack, Reduces incidences of attack, Aborts an impending attack

Mechanism of action: Reduces the inflammation caused by uric acid crystals

Adverse effects: Gastrointestinal, Myelosuppression, Myopathy

Drug interactions: Inhibitor of CYP3A4, Statins

Precautions and contraindications: Older adults, Debilitated patients, Patients with cardiac, renal, hepatic, and GI disease, Pregnant patients

Allopurinol

Action: Reduces blood levels of uric acid, Prevents new tophus formation and causes regression of tophi, Allows joint function to improve, decreases the risk of nephropathy from deposition of urate crystals in the kidney

Uses:Chronic tophaceous gout, Hyperuricemia due to chemotherapy,Hyperuricemia that develops secondary to cancer chemotherapy, Certain blood dyscrasias: Polycythemia vera, myeloid metaplasia, leukemia

Pharmacokinetics: Oral, Eliminated entirely by kidneys, 25 hour half life

Adverse effects:Generally well tolerated, Hypersensitivity syndrome, GI effects, Neurologic effects

Interactions:Warfarin

Probenecid

Action: Acts on renal tubules to inhibit reabsorption of uric acid, Prevents formation of new tophi and helps diminish existing tophi, May exacerbate acute episodes of gout, Add indomethacin for relief

Adverse effects: Usually well tolerated, but mild GI effects occasionally occur; take with food, Risk of kidney damage can be minimized by alkalinizing urine and drinking 2.5 to 3 L of fluid daily during the first few days of treatment

Drug interactions: Aspirin, Other salicylates

Bisphosphonates: Alendronate, Risedronate, Ibandronate, Zoledronate, Pamidronate

Incorporate into bone: Inhibit bone resorption by decreasing activity of osteoclasts

Uses:Postmenopausal osteoporosis, male osteoporosis, glucocorticoid-induced osteoporosis, Paget’s disease of bone

Action:Suppresses resorption of bone

Pharmacokinetics:Oral bioavailability: Poor

Adverse effects: Generally safe, esophageal ulceration, atypical femoral fracture, esophageal cancer, musculoskeletal pain, ocular problems, ONJ, hyperparathyroidism, A-fib

Raloxifene

Selective estrogen receptor modulator (SERM)

Therapeutic uses: Osteoporosis, Breast cancer

Action: Structurally similar to estrogen and binds to estrogen receptors, Comparison to estrogen

Pharmacokinetics: Oral, Metabolized and excreted by liver

Adverse effects:Thromboembolic events, such as deep vein thrombosis (DVT), Pulmonary embolism & stroke, Fetal harm

Amphotericin B

Uses: Drug of choice for most systemic mycoses, Before amphotericin B, systemic fungal infections were usually fatal

Mechanism of action: Binds to ergosterol (much more than cholesterol) in fungal cell membrane (Bacterial cell membranes lack sterols and Fungi damaged more than human cells), Increases permeability, Cell leaks intracellular cations (especially potassium), Fungistatic or fungicidal

Pharmacokinetics: Highly toxic, Infusion reaction and renal damage occur in many patients, Must be given IV; no oral administration

Adverse effects: Infusion reactions, Nephrotoxicity, Hypokalemia, Bone marrow suppression

Infusion reactions: Fever, chills, rigors, nausea, and headache, Caused by release of proinflammatory cytokines, Symptoms begin 1 to 3 hours after start of infusion and last for about 1 hour, Less intense with lipid-based amphotericin B formulations

Mild reactions: Pretreatment options

• Diphenhydramine + acetaminophen

• Aspirin can help but may increase renal damage

IV meperidine or dantrolene can be given if rigors occur

Hydrocortisone can be given with caution

Amphotericin infusion produces a high incidence of phlebitis; this can be minimized by changing peripheral venous sites often, administering amphotericin through a large central vein, and pretreatment with heparin

Fluconazole

Broad-spectrum antifungal agents: Azole

Use: Oropharyngeal candidiasis, Esophageal candidiasis, cryptococcal meningitis, vulvovaginal candidiasis, onychomycosis

Action: Fungistatic, Same mechanism of action as itraconazole

Pharmacokinetics: Oral, Good PO absorption, IV and PO dosage the same, Hepatic metabolism, renal excretion

Adverse effects: Nausea, Headache, Vomiting, Abdominal pain, Diarrhea, Stevens-Johnson syndrome

Caspofungin

Narrow-spectrum antifungal agents: Echinocandins

Mechanism of action: Inhibits the biosynthesis of beta-1,3-d-glucan, an essential component of the cell walls of some fungi (Candida and Aspergillus species)

Use: Invasive aspergillosis in patients unresponsive to or intolerant of traditional agents, Systemic Candida infections

Pharmacokinetics: IV, Half life 9-11 hours, gradual metabolism followed by excretion in the urine and feces.

Adverse effects: generally well tolerated, phlebitis at injection site, headache, rash, nausea, and vomiting, Can cause effects related to histamine release: rash, facial flushing, pruritus, and a sense of warmth

Interactions:Drugs that induce cytochrome P450 (carbamazepine, phenytoin…) may decrease levels of caspofungin, Caspofungin can decrease levels of tacrolimus

Acyclovir

-ciclovir = treatment of herpes simplex virus and varicella-zoster virus infections

Uses: Mucocutaneous Herpes Simplex Infections, Varicella-Zoster Infections, Herpes Simplex Genitalis.

Action: inhibits viral replication by suppressing synthesis of viral DNA

Pharmacokinetics: Oral, topical, IV, Eliminated unchanged by kidneys  

Intravenous therapy: Phlebitis, Reversible nephrotoxicity, Neurotoxicity, Oral therapy: Gastrointestinal, Vertigo, Topical therapy: Stinging sensations

NRTIs (Nucleoside Reverse Transcriptase Inhibitors)

•The NRTIs were the first drugs used against HIV infection

•Are ineffective as monotherapy because resistance develops rapidly

Action: prodrugs that inhibit HIV replication by suppressing synthesis of viral DNA

Adverse effects: Lactic Acidosis, Hepatic Steatosis (Fatty degeneration of the liver), Hepatomegaly (enlarged liver), Pancreatitis

Interactions: Not metabolized by P450 enzymes, few interactions

NNRTIs (Non-Nucleoside Reverse Transcriptase Inhibitors)

•NNRTIs have no structural relationship with naturally occurring nucleosides.

•They are usually combined with an NRTI.

Action: binds to the active center of reverse transcriptase enzyme, causing stereochemical changes, which inhibits DNA replication and promotes premature termination of the growing DNA strand.

Adverse Effects: Generally, no adverse effects shared by NNRTIs, efavirenz and rilpivirine can cause CNS effects

Interactions: multiple drug interactions with commonly

HIV Protease Inhibitors

●Among the most effective antiretroviral drugs, Nine are available, Used in combination with NRTIs; can reduce viral load to an undetectable level, Resistance

Action: prevent HIV maturation by blocking the HIV enzyme protease.

Adverse effects:

• Hyperglycemia/diabetes

• Fat redistribution

• Hyperlipidemia

• Reduced bone density

• Increased bleeding in people with hemophilia

• Reduced bone mineral density

• Elevation of serum transaminase

Enfuvirtide (Fuzeon)

HIV fusion inhibitor

• Widely known as T-20

• First and only HIV fusion inhibitor

Action: Blocks entry of HIV into CD4 T cells

Pharmacokinetics: Twice-daily subQ dosing

Adverse effects: Injection-site reactions, pneumonia, and hypersensitivity reactions

Interactions: Devoid of significant drug interactions

Maraviroc (Selzentry)

CCR5 antagonist

• indicated for combined use with other antiretroviral agents to treat patients aged 16 years and older with particular HIV strains

• a test must be performed to confirm that the infecting HIV strain prior to use

Action: binds with CCR5 and thereby blocks viral entry.

Adverse effects: cough, dizziness, pyrexia, rash, abdominal pain, musculoskeletal symptoms, and upper respiratory tract infections, Liver injury, cardiovascular events (myocardial ischemia and MI)

Interactions: drugs that inhibit or induce CYP3A4 affect maraviroc levels

Filgrastim

Granulocyte colony-stimulating factor (G-CSF)

Stimulates neutrophil production to manage chemotherapy-induced neutropenia around the nadir occurring at days $10\text{--}14$.

Oprelvekin

Thrombopoietic growth factor

Stimulates platelet production to manage chemotherapy-induced thrombocytopenia and prevent bleeding.

Daunorubicin

Antineoplastic chemotherapy agent

Can cause serious injury to the heart

Cisplatin

Antineoplastic chemotherapy agent

Can injure the kidneys

Vincristine

Antineoplastic chemotherapy medication

Can injure peripheral nerves

Inotropic Agents

Dopamine (Intropin): Catecholamine, Activates beta₁-adrenergic receptors in the heart, kidney, and blood vessels, Increases heart rate, Dilates renal blood vessels, Activates alpha₁ receptors

Dobutamine: Synthetic catecholamine, Selective activation of beta₁-adrenergic receptors

Milrinone (Primacor): Inodilator= Increases myocardial contractility and promotes vasodilation, Reserved for patients with severe reduction in cardiac output resulting in decreased organ perfusion, whArrhythmias, myocardial ischemia

Nesiritide

Vasodilator

Principal adverse effect: symptomatic hypotension

Other Class IA: Sodium Channel Blockers

Procainamide (Procanbid): Similar to quinidine PO, Only weakly anticholinergic, Adverse effects: Symptoms of systemic lupus erythematosus

Disopyramide (Norpace): Similar to quinidine PO, Prominent side effects have limited its use

Class IC Agents, Class ll: Beta Blockers, Class IV: Calcium Channel Blockers

IC Agents: Block cardiac sodium channels, Delay ventricular repolarization, All class IC agents can exacerbate existing dysrhythmias and create new ones

• Two class IC agents: Flecainide and Propafenone

Class ll: Beta Blockers = Propranolol, Acebutolol, Esmolol, Sotalol

Class IV: Calcium Channel Blockers = Verapamil & Diltiazem

Bivalirudin (Angiomax)

Direct Thrombin Inhibitor

Therapeutic uses: Prevent clot formation in patients undergoing coronary angioplasty, Patients who have experienced HIT

Pharmacokinetics: IV, renal excretion, 25 minute half life

Adverse Effects: Back pain, nausea, hypotension, headache

Apixaban (Eliquis) & Rivaroxaban (Xarelto)

Other Notable Anticoagulants

No routine INR testing, Rapid onset, short duration, fixed dose, few drug food interactions

Rivaroxaban- should be avoided in renal impairment

Moderate to Strong Opioid Agonists

Codeine

Actions and uses: Pain and cough suppression, 10% converts to morphine in liver

Preparations, dosage, and administration: Usually oral (formulated alone or with aspirin or acetaminophen), 30 mg produces same effect as 325 mg of acetaminophen

Oxycodone [OxyContin, Roxicodone, OxyIR ]

•Analgesic actions equivalent to those of codeine: Immediate-release, Controlled-release [OxyContin]

•Abuse: Crushes and snorts or injects medication

•2010 OP formulation much harder to crush and does not dissolve into an injectable solution to decrease risk of abuse

Hydrocodone

•Most widely prescribed drug in the United States, Combined with aspirin, acetaminophen, or ibuprofen

Tramadol

Nonopioid Centrally Acting Analgesics

Mechanism of action: Combination of opioid and nonopioid mechanisms

Therapeutic use

Adverse effects and interactions

Drug interactions: CNS depressants

Abuse liability

Suicide

Preparations, dosage, and administration: Immediate-release and extended-release

Caphalosporins: Cephalexin, Cefoxitin, Cefotaxime, Cefepime, Ceftaroline

Most widely used group of antibiotics: Beta-lactam antibiotics, Similar to penicillin structure, Bactericidal,Low toxicity

Mechanism of action: Bind to penicillin-binding proteins (PBPs), disrupt cell wall synthesis, and cause cell lysis, Most effective against cells undergoing active growth and division

Resistance from Beta-lactamases (cephalosporinases): First-generation destroyed, Second-generation less sensitive, Third-, fourth-, and fifth-generation agents more resistant than first- and second-generation agents

Adverse effects: Allergy, Bleeding, Thrombophlebitis, dosage reduction in patients with severe renal impairment (except ceftriaxone), Other adverse effects

Interactions: Alcohol, Drugs that promote bleeding, Calcium in neonates

Tetracyclines: Tetracycline, Demeclocycline, Doxycycline, Minocycline, Eravacycline, Omadacycline, Omadacycline

Action: Broad-spectrum antibiotics, Inhibit protein synthesis, bacteriostatic, Increasing bacterial resistance has emerged

Uses:Treatment of Lyme Disease,Treatment of acne, Peptic ulcer disease, Periodontal Disease

Phamacokinetics: Oral and IV, High-dose IV therapy has been associated with severe liver damage, Absorption reduced by food, Metabolized by liver, excreted in urine and bile

Tetracycline and demeclocycline—are eliminated primarily in the urine, they accumulate in patients with kidney disease

Adverse effects: Gastrointestinal irritation, Effects on bone and teeth, Superinfection, Hepatotoxicity, Renal toxicity, Photosensitivity and other effects

Drug and food interaction:

Absorption of tetracyclines is decreased if drug is given with:

○Milk products

○Calcium supplements

○Iron supplements

○Magnesium-containing laxatives

○Most antacids

Increases digoxin and warfarin levels

Sulfonamides: Sulfadiazine, Sulfamethoxazole, Sulfisoxazole

Action: Bacteriostatic, adequate host defenses are essential for the elimination of infection, inhibit the synthesis of folic acid (folate)

Therapeutic uses: Urinary Tract infections, Topical sulfonamides:  superficial infections of the eyes and  suppresses bacterial colonization in burn patients.

Pharmacokinetics: Oral, topical, Metabolized by liver, excreted by kidneys

Microbial resistance: Many bacterial species have developed resistance to sulfonamides, Especially high among gonococci, meningococci, streptococci 

Adverse effects: Hypersensitivity reactions: Stevens-Johnson syndrome, Hematologic effects: glucose-6-phosphate dehydrogenase (G6PD) deficiency, Kernicterus, Renal damage from crystalluria

Drug interactions: Metabolism related, Cross hypersensitivity

Additional Antibacterial Drugs

Bacitracin

• Almost always used topically for bacterial infection

• Systemic; can cause serious toxicity

Polymyxin B

• Topical treatment for ears, eyes, and skin

• Skin treatment usually in combination

• Not used for systemic infection (because of toxicity risk)

Indomethacin [Indocin] & Naproxen [Naprosyn]

NSAIDs

Agents of first choice for acute gouty arthritis

• Better tolerated and more predictable than colchicine

• Relief should be occur within 24 hours; swelling subsides over the next few days

Adverse effects

• Gastrointestinal (GI) ulceration, decreased renal function, fluid retention, increased risk of cardiovascular events

Prednisone

Glucocorticoid

Highly effective in relieving pain

Useful for patients who are hypersensitive to, are unresponsive to, or have medical conditions that contraindicate the use of NSAIDs

Avoid in patients prone to hyperglycemia

Febuxostat [Uloric]

Action: Reduces blood levels of uric acid

Uses: Chronic tophaceous gout

Pharmacokinetics: Oral, Hepatic metabolism, renal excretion

Adverse effects: Liver function abnormalities, Nausea, Arthralgia, Rash

Voriconazole [Vfend]

Broad-spectrum antifungal agents: Azole

Uses: Aspergillosis, Candidemia, Invasive aspergillosis, Esophageal candidiasis, Scedosporium apiospermum–resistant infections

Action: Suppresses synthesis of ergosterol

Pharmacokinetics: Oral and IV, Hepatic metabolism renal excretion

Adverse effects: Hepatotoxicity, Visual disturbances, hallucinations, Teratogenicity, Hypersensitivity reactions, Nausea, vomiting, and abdominal pain, Headache, Drug interactions

Itraconazole [Sporanox]

Broad-spectrum antifungal agent: Azole

Use: Systemic mycoses (alternative to amphotericin B), oral therapy of onychomycosis of the toenails or fingernails

Action: Inhibits the synthesis of ergosterol, inhibits fungal cytochrome P450–dependent enzymes

Pharmacokinetics: Oral, Absorption enhanced by food
and cola, Lower toxicity level, Hepatic metabolism, renal excretion

Side effects: (well tolerated in usual doses), GI effects- Nausea, vomiting, diarrhea, Cardio-suppression (Transient decrease in ventricular ejection fraction), Liver damage

Drug interactions: Can inhibit drug-metabolizing enzymes causing increased levels of many other drugs, Drugs that decrease gastric acidity (antacids, histamine2 (H2) antagonists, and proton pump inhibitors) can greatly reduce absorption of oral itraconazole

Ketoconazole  [Nizoral, Xolgel, Extina]

Mechanism of action: Inhibits ergosterol

Use: Alternative to amphotericin B for systemic mycoses, Oral and topical therapy of superficial mycoses

Pharmacokinetics: Oral and topical, Less toxic and only somewhat less effective, Slower effects, More useful in suppressing chronic infections than in treating severe, acute infections

Adverse effects: generally well tolerated, GI- can be reduced if given with food, Hepatotoxicity- Rare but potentially fatal hepatic necrosis,Other adverse effects- Rash, itching, dizziness, fever, chills, constipation, diarrhea, photophobia, and headache

Griseofulvin [Grifulvin]

Drugs for superficial mycoses:

Uses: Superficial mycoses, Ineffective systemic mycoses

Action: Inhibits fungal mitosis

Pharmacokinetics: Oral, Absorption enhanced by fatty meals, Hepatic metabolism, renal excretion

Adverse effects: Transient headache, Rash, Gastrointestinal effects, insomnia, Tiredness

Drug interactions: Warfarin

Polyene antibiotics: Nystatin [Mycostatin]

Drugs for superficial mycoses:

Use: Used only for candidiasis, Drug of choice for intestinal candidiasis, Also used for candidal infections in skin, mouth, esophagus, and vagina

Action: Binds to ergosterol and disrupt the fungal cell membrane 

Pharmacokinetics: Can be administered orally or topically

GI effects- Nausea vomiting, diarrhea, Local irritation with topical application

Raltegravir and Dolutegravir

Integrase Strand Inhibitors

•Indicated for combined use with other antiretroviral agents to treat adults infected with HIV

Action: target HIV by terminating the integration of HIV into DNA.

Adverse effects:

• Raltegravir- elevation in liver enzymes, insomnia and headache

• Dolutegravir- elevated liver enzymes, hyperglycemia, insomnia, Neutropenia

Interactions:

Raltegravir- does not have as many drug interactions

Dolutegravir- significant interactions with a number of drugs