Unit 4 drugs Flashcards
(42 cards)
Short acting beta 2 agonist
Albuterol inhalation(Proventil HFA, Ventolin HFA, ProAir RespiClick)
Levalbuterol (Xopenex)
Long acting beta 2 agonist
Formoterol (foradil)
Salmeterol(Serevent)
Bronchodilators MOA
Increase cyclic adenosine monophosphate by activation of adenyl cyclase, turning ATP to cAMP. Increased cAMP relaxes bronchial smooth muscle and inhibit release of mediators from mast cells.
Albuterol absorption and distribution
Inhaled: Absorbed in bronchi, low systemic concentration
PO: Well absorbed in GI tract, widely distributed in body fluids and tissue. Unknown about breast milk
Levalbuterol absorption and distribution
Minimally absorbed from respiratory tract and distribution is unknown
Inhaled albuterol metabolism and excretion
Hepatic Metabolism.
Elimination: Renal 90%; Fecal 10%(w/in 24 hours
PO albuterol metabolism and excretion
Hepatic Metabolism.
Elimination: Renal 90%; Fecal 10% (over 3 days)
Levalbuterol Metabolism and excretion
Hepatic Metabolism.
Elimination: Renal 90%; Fecal 10%
Beta 2 agonist side effects
Overuse of the beta2-agonist bronchodilators can lead to seizures, hypokalemia, anginal pain, and hypertension. May have some stimulant-like effects (e.g., increased heart rate, tremors) when they initially begin the medication
Albuterol indication
Bronchospasm associated with asthma or COPD
Levalbuterol indication
Bronchospasm in patients with reversible obstructive airway disease
Formoterol absorption and distribution
inhaled dry powder capsule administered via a unique Aerolizer inhaler. The powdered medication is quickly absorbed in the lungs, with an onset of 1 to 3 minutes. No human studies of distribution into breast milk
Formoterol metabolism and excretion
Hepatic metabolism, renal excretion
Formoterol indication
Long-acting bronchodilator for preventing bronchospasm
Salmeterol absorption and distribution
absorbed via the lungs in small amounts; undetectable amounts are found in the serum with recommended doses. With chronic administration, detected in the serum at very low levels. Is excreted in breast milk in small amounts
Xanthine derivative
Theophylline
Xanthine derivatives MOA
work directly by an unknown mechanism believed to be mediated by selective inhibition of specific phosphodiesterases (PDEs). This produces an increase in cAMP, which then leads to bronchial smooth muscle and pulmonary vessel relaxation.
Theophylline absorption and distribution
Most commonly used in an oral form that is rapidly and completely absorbed from the GI tract. Distributes rapidly in nonadipose tissue and body water, including breast milk and cerebral spinal fluid. Theophylline crosses the placenta.
Theophylline metabolism and excretion
metabolized primarily in the liver, with little or no first-pass effect. Metabolism is believed to occur over multiple parallel pathways, mediated by CYP450. Medications that induce CYP450 can significantly increase clearance of theophylline. CAFFEINE IS MINOR ACTIVE METABOLITE.
Renal excretion
Theophylline ADR
Uncommon with low levels
Theophylline toxicity
Patients who are having signs of toxicity may mistakenly think they have a viral illness. Toxicity symptoms to report include nausea, vomiting, insomnia, jitteriness, headache, rash, severe GI pain, restlessness, convulsions, or irregular heartbeat.
Theophylline indication
Bronchospasm associated with asthma, COPD, and bronchitis
Anticholinergics
Ipatropium bromide(oral inhalant) - Atrovent
Tiotropium(spiriva respimat, spiriva handihaler)
Ipatropium MOA
Block the muscarinic cholinergic receptors by antagonizing the action of acetylcholine. Blocking the cholinergic receptors decreases the formation of cyclic guanosine monophosphate (cGMP), which leads to decreased contractility of the smooth muscle of the lungs