Pharm Exam 3

acetylcsteine (Mucomyst) classification and action

mucolytic
Breaks up linkages or bonds of mucoprotein molecules of respiratory secretions into smaller, more soluble, and less viscous strands
Also effects similar changes in DNA and cellular debris
Most effective at pH 7-9

acetylcsteine ADRs

Few. some N/V, probably due to odor; stomatitis, rhinorrhea
Bronchospasm may occurs in asthmatics

acetylcysteine special information

Has an unpleasant "rotten egg" odor
Wash face after nebulization to remove sticky coating left by drug
Oral (72-hr protocol) or IV infusion (21-hr protocol) - antidote for acetaminophen overdose

guaifenesin (Robitussin) classification and action

Expectorant; bronchomucotropic
Direct irritation of gastric mucosa resulting in referred neural activation of bronchial glands, increased volume and reduced viscosity of respiratory secretions )called gastropulmonary reflex action)

guaifenesin ADRs

Rare; occasional GI irritation

guaifenesin special information

Hydration is very important with any expectorant

epinephrine classification and action

Sympathomimetic (non-selective), bronchodilator
Stimulates alpha, beta-1, and beta 2 receptors
Alpha: mediate vasoconstriction to reduce mucosal edema
Beta-1: stimulates heart rate and force of contraction, as well as cardiac irritability
Beta-2: induces bronchial smooth muscle relaxation

epinephrine ADRs

Nervousness, insomnia, fear, tremors, tachycardia, palpitations, headache, dyspnea

epinephrine special information

Caution with coronary artery disease, hypertension, and hyperthyroidism
If MAO inhibitors used concurrently, will precipitate severe hypertension

isoproterenol (Isuprel) classification and action

Sympathomimetic (non-selective Beta- stim. drug), bronchodilator
Stimulates both beta-1 receptors (which stimulate heart) and beta-2 receptors (which cause bronchodilation and also decrease tone and motility of the GI tract and uterus)

isoproterenol ADRs

Tachycardia and palpitation, headache, nausea, tremor, insomnia
The more it is used, the less effective it may be

isoproterenol special information

Is one of the most powerful bronchodilators

albuterol (Proventil, Ventolin) classification and action

Bronchodilator, sympathomimetic (selective Beta-2 stim)
Beta-2 stimulation, causing relaxation of smooth muscles of bronchial tree and peripheral vasculature
Does have some beta-1 action in high doses

albuterol ADRs

Few. peripheral dilation can cause decreased blood pressure which leads to tachycardia. Also, tremors, nervousness, palpitations, dizziness, headache, N/V, anxiety, lethargy, tinnitus

albuterol special information

An inhaled short-acting beta-2 agonist, or "SABA"
Lasts longer than epinephrine, but onset slightly slower. Use with caution with diabetes, hypertension, cardiac disorders (esp. arrhythmias)
Long-acting beta-2 adrenergic receptor agonists are called "LABAs"
Eg. salmeterol (Servent)

ipratropium (Atrovent) classification and action

Anticholinergic bronchodilator, an inhaled short-acting muscarinic antagonist ("SAAMA")
Blocks cholinergic receptors, reducing bronchial tree. (Does not seem to affect volume or viscosity of sputum)

ipratropium ADRs

Few. Dry mouth, pharyngeal irritation

ipratropium special information

Combivent (ipratropium and albuterol)
Spiriva (tiotropium), tudorza (aclidinium) - same class

aminophylline (Theophylline) classification and action

Bronchodilator, methylated xanthine
Inhibits phosphodiesterase, which allows for increased cAMP - leads to relaxation of smooth muscle (esp. bronchial), stimulates heart, stimulates CNS, and renal excretion. Stimulates medullary respiratory center

aminophylline ADRs

GI: anorexia, N/V (probably due to stim. of vomiting center), abdominal discomfort
CNS: nervousness, insomnia, irritability, headache; severe convulsions and coma
CV: tachycardia; severe - hypotension and arrhythmias
Renal: urinary frequency

aminophylline special information

Half-life in smokers is shorter than in non-smokers
Take with food to decrease GI irritability

aminophylline therapeutic level

8-15 mcg/mL

cromolyn sodium (Intal) classification and action

Antiallergic (histamine inhibitor)
Inhibits release of histamine and other mediators of inflammation
Stabilizes cytoplasmic membrane of mast cells

cromolyn ADRs

Most common one is throat irritation

cromolyn special information

Is used for asthma prophylaxis; has no use in acute attack
Comes in metered dose inhaler (MDI), also power-driven inhaler (turbo-inhaler). Is also a nasal spray (seasonal allergies), and in an ophthalmic solution (allergic eye disorders)
Teach to rinse mouth after inhalation treatment
Especially effective for children (and minimal side effects)
Can prevent exercise-induced asthma attack (use 15 minutes prior)

zafirlukast (Accolate) classification and action

Leukotriene receptor antagonist (LRA)
Competes for leukotriene receptor sites - blocks inflammatory response (bronchoconstriction and inflammatory cell infiltration) caused by leukotrienes

zafirlukast ADRs

GI, headache, elevated liver function tests

zafirlukast special information

Used as maintenance therapy of asthma. Prophylaxis only, not for reversal of bronchospasm in acute attack
Concurrent administration with warfarin causes increased warfarin concentration and elevated PT. administration with aspirin causes increased plasma levels of zafirlukast
Take one hour before meals or two hours afterword

beclomethasone (Vanceril) classification and action

Inhaled corticosteroid (ICS)
Exact mechanism in asthma poorly understood, but does involve suppression of antibody formation
Blocks enzymes which produce inflammatory processes in tissues. (in the endocrine section, we will discuss systemic corticosteroids)

beclomethasone ADRs

Hoarseness, dry mouth, localized thrush infection

beclomethasone special information

Can have some absorption systematically, which then gives a steroid response in the body. Most effective long-term control treatment
Teach client to rinse mouth after use
Combination products
Advair (salmeterol and fluticasone)
Dulera (formoterol and mometasone)
Break (vilanterol and fluticasone)

what is the most effective long-term control treatment (respiratory)?

beclomethasone

dextromethorphan (DM) classification and action

Antitussive, non-opioid
Acts centrally to suppress the medullary cough center (elevates threshold for coughing)
Has NO analgesic or addictive properties

dextromethorphan ADRs

Infrequent. GI distress and drowsiness

dextromethorphan special information

Is synthetic opiate derivative totally devoid of analgesic and respiratory depressant effects (except in overdose)
Many questions about effectiveness now
Is designated "DM" when present with other non-prescription cough medicines

pseudoephedrine (Sudafed) classification and action

Decongestant
Stimulates both alpha and beta adrenergic receptors directly; also causes release of norepinephrine
Cardiac: vasoconstriction and cardiac stimulation (may increase BP)
Respiratory: bronchial muscle relaxation is less prominent than epinephrine
Uterine: reduced activity
CNS: acts as stimulant on cerebral cortex and medulla somethat
Vascular: vasoconstriction (shrinks mucous membranes) but less than epinephrine

pseudoephedrine ADRs

Minimal, though CV = tachycardia, flushing

pseudoephedrine special information

Avoid taking near bedtime as stimulation can occur

diphenhydramine (Benadryl) classification and action

Antihistamine (H1 blocking drug)
Competes with histamine for its receptor sites; thereby preventing physiologic action of histamine
Smooth muscle response to histamine is inhibited. Histamine contracts many muscles (i.e. bronchi and GI) and relaxes others (fine blood vessels)
Vascular: inhibits both vasoconstrictor effects of histamine and, to a degree, the more important vasodilator effects
Capillary permeability: strongly antagonizes action of histamine, this increases capillary permeability and formation of edema and weal
Does not inhibit histamine effect of stimulation of gastric secretion (involves H2 receptors)
Inhibits release of acetylcholine
Sedative

diphenhydramine ADRs

Rarely serious, and often disappear with continues therapy
CNS: sedation, dizziness, tinnitus, lassitude, blurred vision, diplopia, euphoria, nervousness, insomnia
GI: loss of appetite, N/V, epigastric distress, constipation, diarrhea, dry mouth.
Other - urinary frequency, palpitations, hypotension, headache, tingling and weakness of hands (may be caused by Atropine-like action of H1 blockers)
Allergic manifestations may occur - as dermatitis; more with topical application

diphenhydramine special information

Caution: do not take concurrently with alcohol (it enhances sedative effect)
Tolerance can occur
Often used as hypnotic for children and adults

an expectorant drug like guaifenesin is often used to relieve
A) a persistent dry, hacking cough
B) bronchial inflammation
C) vascular congestion
D) chest or upper airway congestion

D) chest or upper airway congestion

the optimal therapeutic range for theophylline (Theo-Dur) is
A) 8-15 mcg/mL
B) 30-35 mcg/mL
C) 2-5 mcg/mL
D) 20-25 mch/mL

A) 8-15 mcg/mL

which of the following is indicated for treatment of an acute asthma attack?
A) beclomethasone (Vanceril)
B) zafirlukast (Accolate)
C) ipratropium (Atrovent)
D) albuterol (Proventil)

D) albuterol (Proventil)

inhaled steroids should be given cautiously to patients with
A) diabetes mellitus
B) hypotension
C) active respiratory infection
D) hypothyroidism

C) active respiratory infection

pseudoephedrine works by
A) mimicking the parasympathetic nervous system
B) mimicking the sympathetic nervous system
C) blocking the parasympathetic nervous system
D) blocking the sympathetic nervous system

B) mimicking the sympathetic nervous system

general lipid guidelines

Total cholesterol < 200 mg/dL
LDL < 100 mg/dL
HDL between 40 and 59 (or higher!)

statins

Highly effective in reducing lipid levels, and are the most prescribed class of anti-lipid drug
Increases HDL modestly, and decrease LDL, total cholesterol, VLDL, and triglycerides

atorvastatin

ADRS are generally mild and fleeting
Potentially serious side effects are
Myopathies
Elevations in liver enzymes
Metabolized by the CYP3A4 enzyme system (the one inhibited by grapefruit juice)
So, drinking the juice may decrease metabolism of atorvastatin and raise its blood levels

anti-hypertensives

BP= CO X TPR
So the BP lowering drugs will attempt to work at multiple places in the body (vessels, heart etc)

alpha 2 agonists

methyldopa (Aldomet) or clonidine
Second line therapy
Inhibit SNS response
Used to decrease withdrawal symptoms from abused substances

alpha 1 blockers

Blocks the vasoconstriction from alpha stimulation- leads to dilation of both arterioles and veins
Also has benefit in BPH- relaxes smooth muscle in bladder neck, prostatic urethra, etc

beta blockers

Can be selective or non selective
Prevents the reflex tachy that you can see with vasodilators
Are also used to decrease cardiac workload (decrease heart rate, cardiac output, etc)

types of vasodilators

Selective to arterioles (hydralazine)
Affect both arterioles and veins (nitroprusside- nipride)

calcium-channel blockers

inhibit the movement of calcium ions across cell membranes; decrease mechanical contraction of the heart
Cause arteriolar dilation, also decrease myocardial contractility, and block renin system
E.g. verapamil (Isoptin, Calan), also diltiazem (Cardizem) and nifedipine (Procardia)
*Nifedipine seems to have little direct action on heart, more on vessels

anti anginals

Nitroglycerin relaxes vascular smooth muscle and both arterial and venous vessels, BUT works mainly on the venous system in those with CAD!!
Dilating veins decrease preload and BP

nitrate tolerance

Particularly likely with topical patches and ointment
Prevented by creating an "nitrate free" period of 10-12 hours per day (often during the night)
ADR
Hypotension and tachy
So check both BP and heart rate before admin

heart failure diuretics

Diuretics reduce the body's fluid volume (help with hypertension, heart failure, cirrhosis, renal disease, increased intraocular pressure, and increased ICP)
Many work to decrease reabsorption of sodium and water along the renal tubule
Degree of diuresis depends on which part of the tubule is affected

diuretics ADRs

Electrolytes other than sodium are affected as well- particularly potassium

hydrochlorothiazide

HCTZ
Thiazide diuretic acts in the distal tubule and increases excretion of sodium chloride potassium and water
ADR mainly due to fluid and electrolyte losses mainly potassium

potassium sparing diuretics

Spironolactone (aldactone)
Works in distal tubule to promote sodium and water excretion BUT also reabsorption of potassium
Weakest diuretic effect if given alone, but works synergistically with other diuretics
Risk for hyperkalemia

osmotic diuretics

Mannitol- a sugar that draws water into the vascular space through osmosis
Filtered in kidney but not reabsorbed- allows for diuresis
ADRs serous fluid and electrolyte disturbances

heart failure contractility

Cardiac glycosides- digoxin (lanoxin)
Strengthens force of myocardial contraction, slows conduction, and slows heart rate
Net effect is increasing cardiac output and controlling rhythm/rate

digoxin

ADRS cardiotoxicity gi and CNS
Antidote- digoxin immune FAB
Monitor electrolyte levels-especially potassium
Hypokalemia increases effects of digoxin- even to toxicity

potassium

Major positively charged ion in the intracellular fluid
Used for prophylaxis with diuretic and/or digoxin therapy
Oral or IV, though NEVER IV push or bolus!

what mediation do you NEVER IV push or bolus?

potassium

antiarrhythmics

Changes in ion currents through the channels of myocardial cell membrane are the main cause of cardiac rhythm changes and arrhythmias (abnormal rhythms)
Any drug used to treat this can cause arrhythmia

quinidine

Class 1A
Treats atrial arrhythmias
Most common ADR is GI disturbance
Most serious ADR is cardiac rhythm changes

lidocaine

Class 1B
Used primarily with ventricular arrhythmias
Very short half life- explains need for continuous IV infusion
Most common ADR affects the heart and CNS

antilipemics

Atherosclerosis- buildup of fatty plaque on the arterial wall
A major cause is excess plasma levels of lipoproteins
Lipoproteins contain a protein shell with core lipid (carriers)
How can we modify (decrease) lipoproteins in the blood?
Modify diet
Drug therapy if dietary changes do not work
VLDL - produced in liver; deliver triglycerides to adipose tissue and muscle
LDL - a by-product of VLDL metabolism; delivers cholesterol to liver and tissues
HDL - removes cholesterol from tissues; has a "good," protective effect
Non-pharmacological ways to alter plasma lipoproteins:
Diet modification (decrease LDL and triglycerides)
Weight loss
Exercise (if sedentary, increases risk)
Smoking (increased LDL and decreased HDL)
DM, hypothyroidism, excessive ETOH ingestion increase risk

drug therapy for reducing cholesterol

There are many groups of drugs with diverse actions
Goal is to decrease LDL without decreasing HDL (keep LDL below100, and HDL 40- 60's)
*Only prophylactic effect, though. None remove existing plaque
Two basic mechanisms of drug effect:
Suppress lipoprotein formation
Accelerate removal

atorvastatin (Lipitor) classification and action

Anti lipid ((HMG-CoA reductase inhibitor)
Inhibits HMG-CoA reductase, the enzyme that catalyzes the rate-limiting step on cholesterol synthesis.

atorvastatin ADRs

Mild, transient GI disturbances, muscle pain, rash, headache, sleep disturbances, increase in serum transaminase levels, peripheral neuropathy, lupus like syndrome, severe myalgia, myositis, and muscle weakness, rhabdomyolysis (muscle breakdown)

atorvastatin special information

Use cautiously in patients who consume large amounts of alcohol, or with known liver disease.
Liver function tests should be monitored at the beginning of therapy, and periodically throughout.
Drugs are contraindicated in pregnancy.
Drugs may enhance the clinical effects of oral anticoagulants.
*Grapefruit juice inhibits the metabolism of statins - toxic levels can occur

medications for hypertension

General approach will likely include a combination of drugs; however, goal is to have drugs work in different ways, not duplicate each other
The Objective is to reduce BP to

methyldopa (Aldomet) classification and action

Sympatholytic antihypertensive, alpha-2 adrenergic agonist
Thought to be central mechanism that reduces sympathetic outflow from brain (medulla). Reduces the amount of NE formed. Result is decreased peripheral resistance. Little or no effect on cardiac output.

methyldopa ADRs

Postural/orthostatic hypotension, sedation, depression, dry mouth, nasal congestion, headache, fever, decreased WBC and platelets, hepatic dysfunction, sexual dysfunction. Na and water retention if not also receiving diuretic.

methyldopa special information

Contraindicated in liver disease or history of major Depression
Sometimes used for pregnancy-induced hypertension (PIH)

prazosin (Minipress) classification and action

Antihypertensive, alpha-1 adrenergic antagonist
Major action is competitive blockade of the alpha-1 adrenergic receptors.
Net result is prevention of constriction by alpha stimulation. Results in vasodilation and decreased peripheral resistance.

prazosin ADRs

Orthostatic hypotension, dizziness, syncope, palpitations, tachycardia, headache, dry mouth, diarrhea, peripheral edema, urinary urgency, impotence.
*"first-dose phenomenon"

atenolol (Tenormin) classification and action

Selective beta adrenergic inhibitor (or "beta-blocker")
Blocks beta-1 adrenergic receptors
Anti-hypertensive effect may be due to:
1. Decreased heart rate and force of contraction
Depresses renin-angiotensin system or
A central action
Anti-anginal: reduction of myocardial oxygen consumption
Anti-arrhythmic; blocks B-adrenergic effect in SA node and Purkinje fibers

atenolol ADRs

CV: bradycardia, CHF, intensify AV block, hypotension
Respiratory: can cause bronchospasm, especially in COPD or asthma
Other: nausea, diarrhea, cramps, fatigue, allergic response

atenolol special information

Check apical and radial pulse and blood pressure before giving
As anti-hypertensive, generally used in combination with a thiazide diuretic and a vasodilator
Used as an antiarrhythmic primarily for supraventricular arrhythmias
BLACK BOX: do not stop abruptly; instead, slowly taper before discontinuing
Use with caution in patients with CHF, asthma, or diabetes
Beta-blockers also used for migraine prophylaxis, MI prophylaxis, panic attacks, benign essential tremor, and PTSD

vasodilators

help reduce BP by acting directly on vascular smooth muscle, and thereby decreasing peripheral resistance

hydralazine (Apresoline) classification and action

Antihypertensive, direct vasodilator
Thought to have direct action on blood vessels, to cause arteriolar vasodilation and increase renal blood flow

hydralazine ADRs

Hypotension, headache, palpitations/tachycardia, anxiety, mild depression, dry mouth, unpleasant taste in mouth, N/V

hydralazine special information

Frequent monitoring in early stages of therapy because of differences in metabolism

verapamil (Calan, Isoptin) classification and action

Calcium antagonist, antianginal, antiarrhythmic
Produces blockade of calcium channels in blood vessels and in heart; effects are:
Arteriolar dilation and resultant lowering BP
Increase in coronary perfusion
SA node causes reduction in heart rate
Decrease in nodal conduction in V node
Decrease in force of myocardial contraction
Inhibition of renin release

verapamil ADRs

Bradycardia, hypotension, severe tachycardia, possible nausea, abdominal discomfort, dizziness, headache, flushing, pruritus, constipation

verapamil special information

Contraindicated in AV block and conditions of reduced myocardial contractility, severe hypotension, and severe CHF
Diltiazem (Cardizem, Tiazac) is similar
Grapefruit juice may increase levels

renin-angiotensin system antagonists

Newer class of drugs (since the 1980's)
Inhibit action of renin-angiotensin-aldosterone system
E.g. captopril (Capoten), enalapril (Vasotec), lisinopril (Zestril); or block receptor - losartan (Cozaar)

lisinopril (Prinivil, Zestril) classification and action

Angiotensin II inhibitor (ACE inhibitor)
Inhibits action of angiotensin-converting enzyme, thereby preventing conversion of angiotensin I to angiotensin II. resulting in:
Reduced vascular tone and a direct lowering of BP
Decreased aldosterone release and less Na retention

lisinopril ADRs

Hypotension, rashes, pruritus, cough, dizziness, headache. Possible hyperkalemia
Rare - neutropenia, agranulocytosis, hepatotoxicity

lisinopril special information

Black box warning: fetal injury and death when taken during pregnancy
Mainstay of therapy for heart failure (see actions)

losartan (Cozaar) classification and action

Angiotensin II receptor antagonist, antihypertensive, ARBs
Blocks binding of angiotensin II to type I receptors in blood vessels and other tissues. Inhibits renin-angiotensin system better and more selectively than ACE inhibitors

losartan ADRs

Dizziness, insomnia, GI, muscle pain and cramps, occasionally increased LFTs. cough probably not an issue

losartan special information

Black box warning: use in pregnancy (because of effects in R-A system)
Maximum effect seen within 3-6 weeks
Losartan with diuretic HCTZ = Hyzaar

angina pectoris

a symptom of transient myocardial ischemia perceived as chest pain or discomfort
"classic" chest pain
- heart is "screaming" for oxygen

nitroglycerin classification and action

Anti-anginal
Relaxation of vascular smooth muscle - exact mechanism is unknown. Peripheral resistance is decreased and venous return to heart is decreased. Net result in decreased and venous return to heart is decreased. Net result in decrease in myocardial oxygen consumption and relief of angina. Note: studies have shown that vessels in the heart of pts with CAD do not dilate in response to NTG

nitroglycerin ADRs

Headache, dizziness syncope, reflex tachycardia, flushing of skin, hypotension