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PharmacologyDrug Stem Drug Class and/or Stem Explanation Examples–alol Combined alpha and beta blockers labetalol, medroxalol–andr– Androgens nandrolone–anserin Serotonin 5–HT(sub)2 receptorantagonistsaltanserin, tropanserin,altanserin–arabine Antineoplastics (arabinofuranosylderivatives)fludarabine...

Description

Pharmacology Drug Stem

Drug Class and/or Stem Explanation

Examples

–alol

Combined alpha and beta blockers

labetalol, medroxalol

–andr–

Androgens

nandrolone

–anserin

altanserin, tropanserin, altanserin fludarabine

–ase

Serotonin 5–HT(sub)2 receptor antagonists Antineoplastics (arabinofuranosyl derivatives) Enzymes

–azepam

Antianxiety agents (diazepam type)

lorazepam

–azosin

Antihypertensives (prazosin type)

doxazosin

–bactam

Beta–lactamase inhibitors

sulbactam

–bamate

Tranquilizers/antiepileptics

meprobamate, felbamate

–barb

Barbituric acid derivatives

phenobarbital

–butazone

mofebutazone

–caine

Anti–inflammatory analgesics (phenylbutazone type) Local anaesthetics

cef–

Cephalosporins

cefazolin

–cillin

Penicillins

ampicillin

–conazole

Antifungals (miconazole type)

fluconazole, oxiconazole

–cort–

Cortisone derivatives

hydrocortisone

–curium

Neuromuscular blocking agents

atracurium

–cycline

Antibiotics (tetracycline type)

minocycline

–dralazine

hydralazine

–erg–

Antihypertensives (hydrazine– phthalazines) Ergot alkaloid derivatives

estr–

Oestrogens

estrone

–fibrate

Antihyperlipidemic

bezafibrate

–flurane –gest–

Inhalation anaesthetics Progestins

enflurane, isoflurane megestrol

–irudin

Anticoagulants

desirudin

–leukin

Interleukin–2 derivatives

teceleukin, aldesleukin

–lukast

Leukotriene antagonists

montelukast, zafirlukast

–mab

Monoclonal antibodies

–mantadine

Antivirals

capromab, daclizumab, detumomab, rimantadine

–monam

Monobactam antibiotics

gloximonam

–mustine

Antineoplastics

carmustine

–mycin

Antibiotics (streptomyces strains)

lincomycin

–olol

Beta–blockers (propranolol type)

timolol, atenolol

–olone

Steroids (no prednisone derivatives)

minaxolone

–oxacin

Antibiotics (quinolone derivatives)

difloxacin, ciprofloxacin

–pamide

Diuretics (sulfamoylbenzoic acid derivatives)

adipamide

–arabine

alglucerase, dornase alfa

–sartan

Angiotensin II receptor antagonists

losartan, eprosartan

–sulfa

Antibiotics (sulfonamide derivatives)

sulfasalazine

–thiazide

Diuretics (thiazide derivatives)

chlorothiazide

–tocin

Oxytocin derivatives

oxytocin, pitocin

–trexate

Antimetabolites (folic acid derivatives)

methotrexate

–triptyline

Antidepressants

amitriptyline

-uracil

Uracil derivatives used as thyroid antagonists and as antineoplastics Antihyperlipidemics (HMG– CoA inhibitors)

fluorouracil

Antiviral substances (undefined group)

viroxime, envirodyne, ganciclovir

–vastatin vir-, -vir- or -vir

lovastatin, simvastatin

Non Non-Steroidal -Steroidal Anti-inflammatory Drugs (NSAIDS) Nonsteroidal anti anti--inflammatory drugs (NSAIDs) provide strong anti-inflammatory and analgesic effects without the adverse effects associated with corticosteroids. These drugs have associated cardiovascular and gastrointestinal risks when taking them. NSAIDs includes propionic acids, acetic acids, fenamates, oxicam derivatives, and cyclooxygenase-2 (COX-2) inhibitors. They differ in chemical structures but NSAIDs are clinically all-inclusive.

dibucaine

Acetaminophen is a related drug which has antipyretic and analgesic properties but does not have the anti-inflammatory effects of the salicylates or the NSAIDs.

Classification NSAIDs and Related Agents Propionic Acids

pergolide

Acetic Acids

Fenamates Oxicam Derivatives

Generic Name fenoprofen flurbiprofen ibuprofen ketoprofen naproxen oxaprozin diclofenac etodolac indomethacin ketorolac nabumetone sulindac tolmetin meclofenamate mefenamic acid meloxicam piroxicam

Disease Spotlight: Primary Dysme Dysmenorrhe norrhe norrheaa •

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Primary dysmenorrhea is defined as cramping pain in the lower abdomen just before or during menstruation, in the absence of other diseases such as endometriosis. (AAFP, 1999) Aetiology is not precisely understood but most symptoms can be attributed to the action of uterine prostaglandin, PGF2a . This stimulates uterine contractions,

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Acetaminophen, a related age the hypothalamus to cause sw mechanism related to analges

Indications • Relief of signs and symptoms • Relief of mild to moderate pa • Treatment of primary dysmen • Fever reduction • Acetaminophen, a related age in children and often used in combination products and ca when taken in high doses. • Acetaminophen is also used in receiving diphtheria–pertussi musculoskeletal pain associat

Pharmacokinetic Pharmacokineticss Route Onset Oral 30 min IV Start of infusio T1/2: -1.8 – 2.5 hrs. Metabolis Metabolism: m: live liverr Excretion: urine

Contraindications and Cautions salicylate licylate • Allergy to NSAIDs or sa • Allergy to sulphonamides. Con • CV dysfunction or hypertensio blee • Peptic ulcer or known GI bleed Pregnancy gnancy o orr lactation. Poten • Pre • Renal or hepatic dysfunction. • Any other known allergies. Ind

Adverse Effects • CNS: headache, dizziness, som • CV: hypertension • GI: nausea, dyspepsia, GI pain • Hema: bleeding, platelet inhib

Interactions • Loop diuretics: decreased diu • Beta-blockers: decreased ant • Ibuprofen: potential for lithiu • Oral anticoagulants: increased • Chronic ethanol ingestion: ris

Adrenergic Antagonists (Sympa (Symp

Adrenergic antagonists are also refer

–pamil –parin

tiapamil heparin, tinzaparin, dalteparin

–peridol

Coronary vasodilators Heparin derivatives and low molecular weight (or depolymerized) heparins Antipsychotics (haloperidol type)

–poetin

Erythropoietin’s

epoetin alfa, epoetin beta

–pramine

Antidepressants (imipramine type)

lofepramine

–pred

Prednisone derivatives

prednicarbate, cloprednol

–pril

Antihypertensives (ACE inhibitors)

enalapril, temocapril, spirapril

–profen

Anti–inflammatory/analgesic agents (ibuprofen type) Antineoplastic antibiotics (daunorubicin type)

flurbiprofen

–rubicin

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ischemia, and sensitization of nerve endings. Prevalence rate is as high as 90 percent and is common among younger women. Some cases are adequately provided relief by OTC NSAIDs.

haloperidol

epirubicin, idarubicin

Therapeutic Act Action ion • Inhibition of prostaglandin synthesis thereby exerting its anti-inflammatory, analgesic, and antipyretic effects. • It blocks two enzymes, namely cyclooxygenase (COX) 1 and 2 present in all tissues and seems to be involved in many body functions, like blood clotting, stomach lining, and sodium-water balance in the kidney. COX-1 turns arachidonic acid into prostaglandins as needed. COX-2 is active at sites of trauma or injury when more prostaglandins are needed. Therefore, NSAIDs block inflammation before all of the signs and symptoms can develop.

the effects of the sympathetic nervo receptor sites without activating the activation.

These drugs occupy the adrenergic r prevented from activating the recept

Adrenergic antagonists have varying five: nonselective adrenergic antago antagonists, and selective alpha1– an

Classification Nonselective Adrener Adrenergic gic Blocking Age Agents nts

Nonselective Alpha Alpha--Adrenergic Blocking Agent Alpha1-Selective Adrenergic Blocking Agents

Nonselective Beta Beta--Adrenergic Blocking Agents

Beta1 Beta1--Selective Adrenergic Blocking Agents

Generic Name amiodarone carvedilol labetalol phentolamine alfuzosin doxazosin prazosin tamsulosin terazosin nebivolol nadolol propranolol timolol bisoprolol esmolol metoprolol

Disease Spotlight: Cardiorespir Cardiorespiratory atory atory--related conditions, Benign Prostatic Hypertrophy •

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Nonselective adrener adrenergic gic antagonists are primarily used to treat cardiac-related conditions. Completely opposite with sympathomimetics, these drugs are ideal for hypertension and heart failure because they reduce the rate and conduction of the heart, relieving it from too much workload. Of all nonselective alpha adr adrenergic energic antagonists, only phentolamine (Regit (Regitine) ine) is used. This drug classification has its use limited because of more specific drugs. Selective alpha1-receptor adrenergic antagonists can improve urine flow in male patients and are used as treatment for benign prostatic hypertrophy (BPH). This is because they can block smooth muscle receptors in the genitourinary tract which leads to relaxation of prostate and bladder. Nonselective beta beta--adrenergic an antagonists tagonists are used to treat CV problems and to prevent reinfarction after MI. Selective beta1 -receptor adrenergic antagonists is more advantageous than nonselective beta-blockers because they don’t block beta2-receptors, allowing bronchodilation. This class is preferred for smokers and those with respiratory problems. They are also used for treating hypertension, angina, and cardiac arrhythmias.

Nonselective Adrenergic Blocking Agents • •

Nonselective adrener adrenergic gic blocking agent agentss block all receptors (alpha- and betareceptors). These drugs are primarily used to treat cardiac-related conditions. Popular example under this class include labetalol and carvedilol.

Therapeutic Action The desired and beneficial actions of nonselective adrenergic antagonists are as follows: • Nonselective adrener adrenergic gic antagonists competitively block the effects of norepinephrine at both alpha and beta receptors throughout the SNS. This results in lower blood pressure, slower pulse rate, and increased renal perfusion with decreased renin levels.

of hypertension) and phentolamine (used during surgery for pheochromocytoma) are two of these drugs. Adults • Adults with diabetes should be monitored closely for fluctuations in glucose levels because sympathetic reactions (e.g. sweating, feeling tense, increased heart rate, and rapid breathing) can cause problems with glucose levels. • Adults with CNS complications may benefit from adrenergic antagonists which are not centrally-acting. • Use of these drugs among pregnant and lactating women is justified when benefits clearly outweigh the risks. Older adults • Dose adjustment is needed as this age group is also more susceptible to drug side effects. • They are more likely to have toxic levels of the drug because of renal or hepatic impairments. • Bisoprolol is the drug of choice for older patients in treating hypertension because it is not associated with as many problems and regular dosing profiles can be used. Pharmacokinetics Route Oral IM T1/2: 6 6--8 h Metabolis Metabolism: m: liver Excretion: urine

Onset Varies Immediate

Peak 1-2 h 5 min

Duration 8-12 h 5.5 h

Contraindications and Cautions • Allergy to any component of the drug. To prevent hypersensitivity reaction • Bradycardia and heart blocks. Can be worsened by slowed heart rate and conduction. impairment. airment. Can alter metabolism of drugs. • Hepatic imp • Asthma Asthma.. Exacerbated by loss of norepinephrine’s effect of bronchodilation. • Shock or heart failure. Can become worse with loss of sympathetic reaction • Lactation. Potential effects on neonates. Advers Adverse e Effects • CNS: dizziness, paraesthesia’s, insomnia, depression, fatigue, vertigo • CV: arrhythmias, hypotension, heart failure, pulmonary oedema, CVA • Respiratory: bronchospasms, cough, rhinitis, bronchial obstruction • GI: nausea, vomiting, diarrhoea, anorexia, flatulence • GU: decreased libido, impotence, dysuria, Peyronie disease. • Others: decreased exercise tolerance, hypoglycaemia, rash • Carvedilol has been associated with hepatic failure related to its effects on the liver. • Abrupt withdrawal: MI, stroke, arrhythmias related to increased hypersensitivity to catecholamines that develops when the receptor sites have been blocked. Interactions halothane hane hane,, isoflurane). Increased risk of • Volatile liquid anaesthetics (e.g. halot excessive hypotension. •

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Assess vital signs, especially p excess stimulation of the card Note respiratory rate and aus effects on bronchi and respira Monitor laboratory test result need for possible dose adjust and appropriateness of thera hypoglycaemia.

Nursing Diagnoses • Decreased cardiac output rela • Ineffective airway clearance r • Risk for injury related to CNS • Diarrhoea related to increase

Implementatio Implementation n with Rationale • Do not discontinue abruptly a catecholamines may develop slowly over two weeks, monit • Educate patient about positiv exercise, smoking cessation) t • Assess heart rate for changes pressure in various positions t • Monitor GI function and need for increased fluid intake rela • Provide comfort measures to • Provide patient education abo enhance knowledge about dr

Evaluation • Monitor patient response to t failure). • Monitor for adverse effects (e • Evaluate patient understandin drug, its indication, and adver • Monitor patient compliance t

Nonselective Alpha Alpha--Adrenergic Bl •

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Nonselective alpha alpha--adrenergic alpha-receptor sites. Their us more specific and safer drugs Of all drugs, only phentolamin

Therapeutic Action • Phentolamine blocks the alph in the vasculature and causing pressure. • It also blocks the alpha2-recep norepinephrine release. The r when blood pressure is lower Indications

Indications adrenergicc antagonists (e.g. labetalol, carvedilol, etc.) are • Most nonselective adrenergi indicated to treat essential hypertension, alone or in combination with diuretics. Others (e.g. amiodarone) is for emergency cases and is only used as an antiarrhythmic. Here are some important aspects to remember for indication of adrenergic antagonists in different age groups: Children • They are at greater risk for complications related to use of these drugs, i.e. bradycardia, difficulty breathing, and changes in glucose metabolism. • Safety of these drugs has not been established in children younger than 18. However, three drugs have established paediatric dosage.Prazosin (for treatment

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Antidiabetics Antidiabetics.. Increased effects of antidiabetics so hypoglycaemia should be watched out for. Verapamil and diltiazem. Potentially dangerous conduction system disturbances if combined with carvedilol.

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Nursing Assessment • Assess for contraindications or cautions (e.g. history of allergy to drug, heart blocks, asthma, pregnancy or lactation status, etc.) to avoid adverse effects. • Establish baseline physical assessment to monitor for any potential adverse effects. • Assess the level of orientation and for any complaints of dizziness, paraesthesia’s, or vertigo to monitor CNS drug effects.

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Phentolamine is most frequen after extravasation of intrave vasodilation and a return of b For treatment of severe hype pheochromocytoma before a For diagnosis of pheochromo

Pharmacokinetic Pharmacokineticss Route IM IV

Onset Rapid Immediate

T1/2: Unknown Metabolis Metabolism: m: Unknown Excretion: Unknown Contraindications and Cautions • Allergy to any component of the drug. To prevent hypersensitivity reaction • Coronary artery disease or MI. Potential exacerbation of these conditions. • Pregnancy and lactation. Potential effects to foetus or neonates. Adverse Effects • CNS: headache, weakness, dizziness • CV: hypotension, orthostatic hypotension, angina, MI, cerebrovascular accident, flushing, tachycardia, arrhythmia • GI: nausea, vomiting, diarrhoea Interactions • Ephedrine and epinephrine. Decreased hypertensive and vasoconstrictive effects • Alcohol. Increased hypotension Nursing Assessment • Assess for contraindications or cautions (e.g. history of allergy to drug, CV diseases, pregnancy or lactation status, etc.) to avoid adverse effects. • Establish baseline physical assessment to monitor for any potential adverse effects. • Assess orientation, affect, and reflexes to monitor for CNS changes related to drug therapy. • Monitor CV status (blood pressure, pulse rate, peripheral perfusion) to determine changes in function. • Monitor urine output which will reflect perfusion of the kidney as another assessment of cardiac function. Nursing Diagnoses • Decreased cardiac output related to blood pressure changes, arrhythmias, and vasodilation • Risk for injury related to CNS and CV effects Implementatio Implementation n with Rationale • Monitor heart rate and blood pressure closely and frequently for changes to anticipate the need to discontinue the drug if adverse reactions are severe. • Inject phentolamine directly into area of extravasation of epinephrine or dopamine to prevent local cell death. • Institute safety measures to prevent injury if the patient experiences weakness, dizziness, or orthostatic hypotension. • Provide comfort measures to help patient cope with drug effects. • Provide patient education about drug effects and warning signs to report to enhance knowledge about drug therapy and promote compliance. Evaluation • Monitor patient response to therapy (improvement in signs and symptoms of pheochromocytoma, improvement in tissue condition after extravasation). • Monitor for adverse effects (e.g. orthostatic hypotension, arrhythmias, CNS effects).

Therapeutic Action • Blocking the postsynaptic alpha1-receptor sites. This causes a decrease in vascular tone and vasodilation, which leads to a fall in blood pressure. A reflex tachycardia that accompanies a fall in blood pressure does not occur because they do not block presynaptic alpha2-receptor sites. • Reducing total peripheral resistance through alpha blockade; it does not affect heart rate or cardiac output. • Increasing high-density lipoproteins while lowering total cholesterol level. • Blocking smooth muscle receptors in prostate, prostatic capsule, prostatic urethra, and urinary bladder neck leading to relaxation of bladder and prostate and improved flow of urine in male patients.

Implementatio Implementation n with Rationale • Monitor blood pressure, pulse for changes that may indicate effects are severe. • Establish safety precautions if prevent patient injury. • Arrange for small, frequent m maintain nutrition. • Provide comfort measures to • Provide patient education abo enhance knowledge about dr

Indications • For trea...