| Drug:
Epinephrine or Adrenalin
(generic) |
| Drug Class: Sympathomimetic |
| Mechanism of Action: in asthma it
induces beta-2 mediated bronchodilation.
It also has alpha-mediated effects
that can constrict bronchial vessels, thus reducing
fluid congestion. |
| Indications: 1) treatment of acute
hypersensitivity (anaphylactoid reactions
to drugs, animal serums and other allergens), 2) treatment of acute
asthmatic attacks to relieve bronchospasm not controlled
by inhalation or subcutaneous administration of other solutions of the drug,
and 3) treatment and prophylaxis of cardiac arrest and attacks of transitory
atrioventricular (A-V) heart block with syncopal seizures (Stokes-Adams
Syndrome). |
| Side Effects: unwanted cardiovascular
side effects due to beta-1 and alpha-1 & 2 stimulation (increased heart
rate, blood pressure). |
| References: www.rxlist.com
& Katzung's text |
| Drug: Albuterol
(generic, Proventil, Ventolin ®) |
| Drug Class: Beta-2 Selective Sympathomimetic |
| Mechanism of Action: Stimulates beta-2
adrenergic receptors, causing an increase in cAMP levels & bronchodilation |
| Indications: the prevention and relief
of bronchospasm in patients with reversible obstructive airway disease and
for the prevention of exercise-induced bronchospasm. |
| Pharmacokinetics: oral or inhalant
administration. Some degree of tolerance may develop with chronic use (loss
of bronchoprotective action). |
| Side Effects: reflex tachycardia |
| References: www.rxlist.com
& Katzung's text |
| Drug: Ipratroprium
bromide (Atrovent ®) |
| Drug Class: antimuscarinic bronchodilator |
| Mechanism of Action: a quaternary
derivative of atropine. The degree of muscarinic
involvement in bronchomotor responses varies amongst patients.
In some patients only a modest relief of bronchoconstriction can be produced,
while in others it can be quite effective. |
| Indications: administered either alone
or with other bronchodilators, especially beta adrenergics, is indicated
as a bronchodilator for maintenance treatment
of bronchospasm associated with chronic obstructive pulmonary
disease, including chronic bronchitis and emphysema. |
| Contraindications: should be used
with caution in patients with narrow-angle glaucoma, prostatic hypertrophy
or bladder-neck obstruction. |
| Pharmacokinetics: can be delivered
in high doses to muscarinic receptors in the airways because it is poorly
absorbed and does not readily enter into the CNS. |
| Side Effects: few |
| References: www.rxlist.com
& Katzung's text |
| Drug: Beclamethasone
(QVAR, Vanceril ®), Budesonide
(Pulmicort ®), Fluticasone (Flovent
®) |
| Drug Class: Coritcosteriods |
| Mechanism of Action: Inhibit phospholipase
A2 and thereby inhibit the production of inflammatory
cytokines. They do not relax airway smooth muscle directly,
but reduce bronchial reactivity. Their effect may be due in part to potentiating
the effects of beta agonists, but their most important action is to inhibit
the lymphocytic and eosinophilic mediated airway inflammation in asthmatics.
Corticosteroids are not curative. |
| Indications: routinely prescribed
for patients who require more than occasional
inhalations of a beta-2 agonist for relief of symptoms.
|
| Pharmacokinetics: aerosol treatment
is the most effective way to decrease systemic adverse effects of corticosteroid
therapy when treating asthmatic patients. |
| References: Katzung's text |
| Drug: Theophylline
(generic, Elixophyllin, Slo-Phyllin, Theo-Dur, Theo-24 ®) |
| Drug Class: Methylxanthine |
| Mechanism of Action: produces direct
bronchodilation and has some anti-inflammatory actions in the airway. At
therapeutic doses theophylline inhibits cell
surface receptors for adenosine. These receptors modulate
adenyl cyclase activity, and adenosine can cause contraction of airways
and provoke histamine release from mast cells. At high concentrations methylxanthines
can also inhibit phosphodiesterase, thereby elevating cAMP. |
| Indications: treatment of the symptoms
and reversible airflow obstruction associated with chronic asthma and other
chronic lung diseases, e.g., emphysema and chronic bronchitis. |
| Pharmacokinetics: Theophylline should
only be used where methods to measure blood levels are available due to
its narrow therapeutic index.
Therapeutic levels range from 5-20 mg/L, and levels above 40 mg/L may cause
seizures or arrhythmias. Theophylline is metabolized by the liver with plasma
clearance that can be effected by liver disease, cigarette smoking, or by
changes in diet. Children clear theophylline faster than adults. |
| Side Effects: Low doses - mild cortical
arousal & deferral of fatigue. High doses - convulsions, cardiac arrhythmias,
death. Because of the high morbidity and mortality associated with theophylline-induced
seizures, treatment should be rapid and aggressive. The initial treatment
for seizures is i.v. diazepam. Repetitive seizures are treated with phenobarbital.
The doses of these drugs required to treat theophylline induced seizures
may be close to those causing respiratory arrest. |
| Major drug interactions: the
list is long (see reference) |
Notes: Aminophylline is a theophylline-ethylenediamine
complex. Theophylline can be taken orally, and it's low cost makes it
attractive for economically disadvantaged patients with societies where
health care resources are limited. |
| References: www.rxlist.com
& Katzung's text |
| Drug: Cromolyn
sodium (generic, Intal ®) and Nedocromil
sodium (Tilade ®) |
| Drug Class: Asthma medication |
| Mechanism of Action: believed to act
by altering the function of delayed chloride channels in the cell membrane
to produce an inhibitory effect on mast cells
and eosinophils that prevents the release of cell mediators.
The inhibitory effect on mast cells appears to be specific for those in
the lung, and explains its ability to blunt the early response to antigen
challenge. Its effect on eosinophils is responsible for inhibiting the inflammatory
response to inhaled allergens. |
| Indications: a prophylactic
agent indicated in the management of patients with bronchial
asthma |
| Pharmacokinetics: inhaled in metered
doses. Poorly absorbed. |
| Side Effects: minor and few, localized
throat irritation |
| References: www.rxlist.com (
Cromolyn
& Nedoromil)
& Katzung's text |
| Drug: Phenylephrine
(generic, Neo-Synephrine ®) |
| Drug Class: Nasal decongestant |
| Mechanism of Action: alpha1 selective
adrenergic agonist |
| Indications: reduce
the discomfort of hay fever and, to a lesser extent, the
common cold by decreasing the volume of the nasal mucosa. |
| Pharmacokinetics: commonly applied
as the active ingredient in a nasal spray.
Phenylephrine is unpredictably absorbed from the GI tract if taken orally. |
| Side Effects: rebound hyperemia. Repeated
topical use may cause ischemic changes in the mucous membranes. |
| Notes: Other formulations of phenylephrine
can also be given systemically to raise blood pressure in hypotensive states
(e.g. during spinal anesthesia or shock like states). |
| References: Katzung's text |
| Drug: Pseudoephedrine
(generic, Sudafed ®) |
| Drug Class: Nasal decongestant |
| Mechanism of Action: similar to ephedrine
- has both an alpha and beta agonist properties,
and to act as an indirectly acting agaonist (tyramine like
effect). Alpha receptor effects in the respiratory mucosa produces vasoconstriction,
which shrinks swollen nasal mucous membranes; reduces tissue hyperemia,
edema, and nasal congestion; and increases nasal airway patency. Also, drainage
of sinus secretions is increased, and obstructed eustachian ostia may be
opened. |
| Indications: relief of nasal congestion
or eustachian tube congestion. |
| Contraindications: patients taking
MAO inhibitors. Use with
caution in patients with hypertension or men with prostatic enlargement.
|
| Pharmacokinetics: oral decongestants
have a prolonged duration of action,
but do not achieve as high local concentrations compared to topical agents
administered in nasal sprays |
| Side Effects: oral decongestants cause
more systemic effects, including nervousness & insomnia compared to
topical agents. It has peripheral effects similar to epinephrine and central
effects similar to, but less intense than, amphetamines. At the recommended
oral dosage, it has little or no pressor effect in normotensive adults.
|
Notes: pseudoephedrine is an isomer
of ephedrine that is less potent in terms of producing tachycardia, increased
blood pressure & CNS stimulation. |
| References: www.rxlist.com
, & Katzung's text |
| Drug: Oxymetazoline
(generic, Afrin, Neo-Synephrine 12 Hour ®) |
| Drug Class: Long- Acting Topical
Nasal Decongestant |
| Mechanism of Action: direct acting
alpha agonist (1 & 2) |
| Indications: for the temporary relief
of nasal (of the nose) congestion or stuffiness caused by hay fever or other
allergies, colds, or sinus trouble. |
| Contraindications:concomitant
use of MAO Inhibitors |
| Pharmacokinetics: Long
acting topical decongestant |
| Side Effects: in large doses it may
produce hypotension due to a CNS clonidine like effect |
Notes: oxymetazoline is also found
in some formulations of Visine ® |
| References: Katzung's text |
| Drug: Codeine
(generic) |
| Drug Class: Antitussive, narcotic
analgesic |
| Mechanism of Action: unclear. The
physiological mechanism of cough is complex, and little is known about the
specific mechanism of action of the opioid antitussive drugs. The receptors
involved appear to be different than those involved with the other actions
of opioids. It is likely that both central & peripheral effects may
play a role. |
| Indications: opioid analgesics are
amongst the most effective drugs for suppression of cough. |
| Contraindications: use with caution
in patients on MAO inhibitors |
| Pharmacokinetics: Taken orally. Low
doses (tablets or syrup) are sufficient to relieve cough |
| Side Effects: Cough suppression by
opioids may allow accumulation of secretions and lead to airway obstruction.
Other possible side effects: constipation, drowsiness, nausea/vomiting,
addictive potential. |
| References: Katzung's text |
| Drug: N-acetylcysteine
(Mucomyst ®) |
| Drug Class: Mucolytic |
| Mechanism of Action: used as a mucolytic
("mucus dissolving") agent to help break up the thick mucus often
present in people suffering from chronic respiratory ailments. It opens
disulfide bonds, reducing the viscosity of mucous. Dilution of thick mucus
makes it easier to cough up, or drain, from the nasal passages and other
congested areas. |
Indications: to reduce congestion
related to sinusitis, bronchitis, asthma, and other respiratory diseases.
It's often used to ease congestion in people with pneumonia and other
chronic respiratory diseases. |
Notes: also used in the treatment
of acetaminophen overdose |
| Drug: Dornase
alpha (Pulmozyme ®) |
| Drug Class: Treatment of Cystic
Fibrosis |
| Mechanism of Action: Dornase alpha
is a genetically engineered form of the human enzyme, deoxyribonuclease
or DNAse. Dornase alpha breaks
down the DNA and thereby reduces the thickness of the fluids in the lungs
of patients with cystic fibrosis (see Notes). |
| Indications: treatment of cystic
fibrosis, the most common fatal genetic disease in developed
countries. |
Notes: The lungs continually secrete
fluid into the airways to keep them moist. In cystic fibrosis, the fluid
becomes thick because the amount of water it contains is reduced. The
thickened fluid is difficult to cough up or spit out. It blocks the airways,
making breathing difficult and promoting the growth of bacteria and infection.
Infection destroys the tissues of the lungs, and it is the slowly progressive
destruction of the lungs that is the major cause of disability and death
in children with cystic fibrosis. The thick fluid contains high concentrations
of deoxyribonucleic acid (DNA). |
| References: www.medicine.net |
| Drug: Isoniazid
or INH (generic) |
| Drug Class: Antimycobacterial (anti-tuberculosis) |
| Mechanism of Action: Inhibits biosynthesis
of mycolic acids which are important for mycobacterial cell wall synthesis;
bactericidal in dividing cells. Bacteriostatic in resting cells. |
| Indications: subsceptible strains
of tuberculosis |
| Contraindications: isoniazid drug
hypersensitivity including drug -induced hepatitis; previous isoniazid-associated
hepatic injury. |
| Side Effects: Isoniazid induced hepatic
toxicity is the most frequent major toxic effect. 10-20% of patients develop
a peripheral neuropathy (that can be minimized with simultaneous administration
of pyridoxine). Isoniazid can induce hemolytic anemia in G-6-P dehydrogenase
deficiency. |
| Pharmacokinetics: Well absorbed orally.
Widely distributed in various tissues. Metabolized in liver-acetylation,
renal excretion. Plasma half-life in fast acetylators is 70 min and in slow
acetylators is 2-5 hr. |
| Major drug Interactions: |
| Notes: Severe and sometimes fatal
hepatitis associated with isoniazid therapy has been reported and may occur
or may develop even after many months of treatment. The risk of developing
hepatitis is age related. |
| Reference: www.rxlist.com |
| Drug: Rifampin
(generic, Rifadin, Rimactane ® ) |
| Drug Class: Antimycobacterial |
| Mechanism of Action: Inhibits RNA
synthesis by inhibiting DNA dependent RNA polymerase; bactericidal |
| Indications: administered along with
isoniazid, ethambutol or another antituberculosis drug to prevent the emergence
of drug-resistant myocbacteria. Also used to treat infections by Gram+ and
Gram-cocci, Methicillin resistant Staph; Gram- organisms- Legionella, H.
influenzae. |
| Contraindications: history of rifampin
hypersensitivity |
| Side Effects: Orange-red colored urine
and feces, rash. |
| Pharmacokinetics: Well absorbed orally.
Widely distributed, enterohepatic circulation, deacetylation, biliary excretion.
|
| Major drug Interactions: Rifampin
is a strong inducer of P-450 enzymes, which increases the elimination of
other drugs including anticoagulants, some anticonvulsants, protease inhibitors
and contraceptives. |
| Reference: Katzung's text |
| Drug: Ethambutol
(Myambutol ®) |
| Drug Class: Antimycobacterial |
| Mechanism of Action: Inhibits synthesis
of arabinogalactan, an essential component of mycobacterial cell wall. Bacteriostatic.
Enhances the activity of lipophilic drugs such as rifampin. |
| Indications: administered along with
isoniazid or rifampin to inhibit the growth of M. tuberculosis and other
susceptable mycobacteria. |
| Contraindications: |
| Side Effects: Optic neuritis resulting
in decrease of visual acuity and loss of ability to differentiate red from
green. |
| Pharmacokinetics: Well absorbed orally.
Metabolized partially to a dicarboxylic acid derivative. 75% excreted unchanged
in urine. |
| Reference: Katzung's text |
| Drug: Pyrazinamide
(generic) |
| Drug Class: Antimyocobacterial |
| Mechanism of Action: Inhibits electron
transport in mycobacteria. Exact mode of action not known. Mycobacterial
fatty acid synthase I gene invovlved in mycolic acid biosynthesis may be
a target. Bactericidal. |
| Indications: used along with isoniazid
and rifampin for short course (e.g. 6 month) regimens as a"sterilizing"
agent against residual intracellular organisms that may cause a relapse
of infection by tubercle bacilli. |
| Side Effects: hepatotoxicity (1-5%),
nausea, vomiting, hyperuricemia |
| Pharmacokinetics: Well absorbed orally.
Distributed widely. Hydrolyzed to pyrazinoic acid. Renal excretion. |
| Reference: Katzung's text |
| Drug: Clofazimine
(Lamprene ®) |
| Drug Class: Antimycobacterial (Leprosy drug) |
| Mechanism of Action: binds to DNA
and inhibits template function; weak bactericidal. |
| Indications: an alternative to dapsone
(sulfone) for treating resistant leprosy or patients intolerant to dapsone. |
| Side Effects: Red colored urine. Nausea
vomitting, diarrhea and abdominal pain, red brown pigmentation of skin. |
| Pharmacokinetics: Absorbed orally
45-62%. Deposits in fatty tissues. Biliary excretion. Red colored urine.
|
| Reference: Katzung's text |
| Drug:Clarithromycin
(Biaxin ®) |
| Drug Class: Macrolide antibiotic |
| Mechanism of Action: binds to the
50S ribosomal subunit of susceptible microorganisms and inhibits the translocation
step, resulting in inhibition of protein synthesis. Clarithromycin is active
in vitro against a variety of aerobic and anaerobic gram-positive and gram-negative
microorganisms as well as most Mycobacterium avium complex (MAC) microorganisms. |
| Indications: disseminated mycobacterial
infections due to Mycobacterium avium, or Mycobacterium intracellulare.
Treatment of mild to moderate infections caused by susceptible strains of
the designated microorganisms in the conditions: Pharyngitis/Tonsillitis
due to Streptococcus pyogenes (but the usual drug of choice is a penicillin);
Acute maxillary sinusitis due to Haemophilus influenzae or Streptococcus
pneumoniae; Acute bacterial exacerbation of chronic bronchitis due to Haemophilus
influenzae, or Streptococcus pneumoniae; Pneumonia due to Mycoplasma pneumoniae,
Streptococcus pneumoniae, or Chlamydia pneumoniae (TWAR). |
| Contraindications: hypersensitivity
to any of the macrolide antibiotics. Concomitant administration of clarithromycin
with pimozide, or other drugs that prolong the QT interval is contraindicated
due to likelihood of producing a long QT syndrome & arrhythmias |
| Side Effects: diarrhea, nausea |
| Pharmacokinetics: Clarithromycin is
rapidly absorbed from the gastrointestinal tract after oral administration.
The absolute bioavailability of 250-mg clarithromycin tablets was approximately
50%. |
| Major drug Interactions: |
| Reference: www.rxlist.com |
| Drug: Thalidomide
|
| Drug Class: Antimycobacterial (Leprosy drug) |
| Mechanism of Action: Thalidomide is
an immunomodulatory agent with a spectrum of activity that is not fully
characterized, but may involve downregulation of both TNF-alpha and adhesion
moleucules involved in leukocyte migration. |
| Indications: for the acute treatment
ofthe cutaneous manifestations of moderate to severe erythema nodosum leprosum
(ENL) |
| Contraindications: IF THALIDOMIDE
IS TAKEN DURING PREGNANCY, IT CAN CAUSE SEVERE BIRTH
DEFECTS OR DEATH TO AN UNBORN BABY. THALIDOMIDE SHOULD NEVER
BE USED BY WOMEN WHO ARE PREGNANT OR WHO COULD BECOME PREGNANT WHILE TAKING
THE DRUG. |
| Side Effects: The most serious toxicity
associated with thalidomide is its documented human teratogenicity |
| Major drug Interactions: Medications
known to be associatedwith peripheral neuropathy should be used with caution
in patients receiving thalidomide. Thalidomide has been reported to enhance
the sedative activity of barbiturates, alcohol, chlorpromazine, and reserpine. |
| Reference: www.rxlist.com |
