Chapter 36 Antihistamines, Decongestants, Antitussives, and Expectorants Flashcards
Common colds result from a viral infection, most often
infection with a rhinovirus or an influenza virus. These
viruses invade the tissues (mucosa) of the upper respiratory tract (nose, pharynx, and larynx) to cause an?
upper respiratory tract infection (URI).
Many antihistamines, nasal decongestants, antitussives, and expectorants are available without prescription. These drugs can?
only relieve the symptoms of a URI; they can do nothing
to eliminate the causative pathogen.
Antiviral drugs are currently the only drugs that are effective for URIs; however, treatment with these medications is often hampered by the fact that the viral cause cannot be readily identified. The treatment rendered can only be based on what is believed to be the most likely cause, given the presenting clinical symptoms. This is known as?
empiric therapy.
Histamine is a substance that performs many functions. It is involved in?
1) nerve impulse transmission in the central nervous system (CNS) 2) dilation of capillaries 3) contraction of smooth muscle 4) stimulation of gastric secretion 5) acceleration of the heart rate.
During allergic reactions, histamine and other substances are released from?
mast cells, basophils, and other cells in response to antigens circulating in the blood. Histamine molecules
then bind to and activate other cells in the nose, eyes, respiratory tract, gastrointestinal (GI) tract, and skin, producing the characteristic allergic signs and symptoms.
There are two types of histamine blockers: H1 blockers and H2 blockers
- H1 blockers are the drugs to which most people
are referring when they use the term antihistamine. H1 blockers prevent the harmful effects of histamine and are used to treat seasonal allergic rhinitis, anaphylaxis, reactions to insect bites, and so forth. - H2 blockers are used to treat gastric acid disorders, such as hyperacidity or ulcer disease and include cimetidine (Tagamet), ranitidine (Zantac), famotidine
(Pepcid), and nizatidine (Axid).
H1 antagonists include drugs such as diphenhydramine
(Benadryl), chlorpheniramine (generic), fexofenadine
(Allegra), loratadine (Claritin), and cetirizine (Zyrtec). They
are of greatest value in the treatment of?
nasal allergies, particularly seasonal hay fever.
-also have palliative, not curative effects such as relieving the symptoms of the common cold such as sneezing and running nose
H-1 Receptor
Mediate smooth muscle contraction & dilation of capillaries
The clinical efficacy of the different antihistamines is very
similar, although they have varying degrees of?
antihistaminic, anticholinergic, and sedating properties.
Antihistamines affect the secretions of?
Lacrimal, salivary, and respiratory mucosal glands, which are the primary anticholinergic actions of antihistamines
Antihistamines differ from each other in their?
Potency and adverse effects, especially in degree of drowsiness they produce
- the antihistaminic, anticholinergic, and sedative properties, they are indicated for tx of allergies
- They are also useful for the treatment of problems such as vertigo, motion sickness, insomnia, cough, and are sometimes used as sleep aids.
Antihistamines mechanism of action
Block the histamine receptors on the surfaces of basophils and mast cells, thereby preventing the release and actions of histamine stored within these cells. They do NOT push off histamine that is already bound to receptors but compete with histamine for unoccupied receptors. Therefore they are most beneficial when given early in a histamine-mediated reaction before all of the free histamine molecules bind to cell membrane receptors. The binding of H1 blockers to these receptors prevents the adverse consequences of histamine binding: vasodilation; increased GI, respiratory, salivary, and lacrimal secretions; and increased capillary permeability with resultant edema.
Antihistamines Contraindications
Antihistamines are not to be used as the sole drug therapy during acute asthmatic attacks. In such cases, a rapidly acting bronchodilator such as albuterol, or in extreme cases epinephrine, is the most urgently needed medication.
- narrow angle glaucoma, cardiac disease, kidney disease, HTN, bronchial asthma, COPD, peptic ulcer disease, seizure disorders, BPH, pregnancy
- used in caution w/pts that have impaired liver function or renal insufficiency, as well as lactating women
Antihistamines Adverse effects
Drowsiness is usually the chief complaint of people who take antihistamines.
-the anticholinergic (drying) effects: dry mouth, changes in vision, difficulty urinating, constipation
Antihistamine Drug: Diphenhydramine (Benadryl)
- works peripherally & centrally
- anticholinergic & sedative effects
- hypnotic drug (sedative effects)
- not advised in older adults due to “hangover” effect & increased potential for falls
- excellent safety profile and efficacy
- greatest range of therapeutic indications
- used for relief/prevention of histamine-related allergies, motion sickness, Parkinson’s disease (anticholinergic effects)
- used in conjunction with epinephrine in management of anaphylaxis & Tx of acute dystonic reactions
- Pregnancy category b
- use w/caution in: nursing mothers neonates, & pt’s w/lower respiratory tract symptoms
- oral, parenteral, topical
A major advance in antihistamine therapy occurred with the development of the nonsedating antihistamines loratadine, cetirizine, and fexofenadine. These drugs were developed to eliminate many of the unwanted sedative effects of the older antihistamines. These drugs work peripherally to block the actions of histamine and therefore have significantly fewer CNS effects than many older antihistamines. For this reason, these drugs are also called peripherally acting antihistamines because they do not readily cross the blood-brain barrier.
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Nasal congestion is due to excessive nasal secretions and inflamed and swollen nasal mucosa. The primary causes of nasal congestion are?
allergies and URIs, especially the common cold.
Decongestants work by?
causing constriction of the engorged and swollen blood vessels in the sinuses, which decreases pressure and allows mucous membranes to drain. It is important to understand the action of these drugs and know other important information such as significant adverse effects, including cardiac and CNS-stimulating effects.
There are three separate groups of nasal decongestants:
(1) adrenergics (sympathomimetics), which are the largest group
(2) anticholinergics (parasympatholytics), which are somewhat less commonly used
(3) selected topical corticosteroids (intranasal steroids).
Nasal decongestants are most commonly used for their ability to shrink engorged nasal mucous membranes and relieve nasal stuffiness. Adrenergic drugs (e.g., ephedrine, oxymetazoline) accomplish this by?
constricting the small arterioles that supply the structures of the upper respiratory tract, primarily the blood vessels surrounding the nasal sinuses.
Nasal decongestants reduce the nasal congestion associated with?
acute or chronic rhinitis, the common cold, sinusitis, and hay fever or other allergies. They may also be used to reduce swelling of the nasal passages and to facilitate visualization of the nasal and pharyngeal membranes before surgery or diagnostic procedures.
The clinical problem of rebound congestion associated with topically administered drugs is almost nonexistent with oral dosage forms. Rebound congestion occurs because of the?
very rapid absorption of the drug through mucous membranes followed by a more rapid decline in therapeutic activity. This can cause addiction to the nasal spray, as patients take it frequently due to the rapid decline in activity.
Inhaled intranasal steroids and anticholinergic drugs are not associated with rebound congestion and are often used?
prophylactically to prevent nasal congestion in patients with chronic upper respiratory tract symptoms.
Nasal steroids are aimed at the?
inflammatory response elicited by invading organisms (viruses and bacteria) or other antigens (e.g., allergens).
- Steroids exert their antiinflammatory effect by causing these cells to be turned off or rendered unresponsive
- goal is NOT complete immunosuppression of the respiratory tract but rather to reduce the inflammatory symptoms to improve patient comfort and air exchange
Decongestants contraindication
- Adrenergic drugs are contraindicated in narrow-angle glaucoma, uncontrolled cardiovascular disease, hypertension, diabetes, hyperthyroidism, and prostatitis and in situations in which the patient is unable to close his or her eyes (such as after a cerebrovascular accident), as well as in patients with a history of cerebrovascular accident or transient ischemic attacks, cerebral arteriosclerosis, long-standing asthma, benign prostatic hyperplasia, or diabetes.
Decongestants Adverse effects
Adrenergic drugs are usually well tolerated. Possible adverse effects of these drugs include nervousness, insomnia, palpitations, and tremor. The most common adverse effects of intranasal steroids are localized and include mucosal irritation and dryness.
Decongestants interactions
Systemic sympathomimetic drugs and sympathomimetic nasal decongestants are likely to cause drug toxicity when given together.
- MAOIs may result in additive pressor effects (raising BP) when given with sympathomimetic nasal decongestants
- methyldopa & urinary acidifiers and alkalinizers