COUGH AND COLD PREPARATIONS

ANTIHISTAMINEDiphenhydramine

DECONGESTANTS MUCOLYTICS

Acetylcysteine EXPECTORANTS

Guaifenesin COUGH SUPPRESSANTS

CodeineDM (dextromethorphan)

Global Strategy for the Diagnosis, Management, and Prevention of Chronic Obstructive Pulmonary Disease NHLBI/WHO Global Initiative for Chronic Obstructive Lung Disease (GOLD) Workshop Summary 2008

Mucolytic (mucokinetic, mucoregulator) agents. (ambroxol, erdosteine, carbocysteine, iodinated glycerol): Although a few patients with viscous sputum may benefit from mucolytics (124, 125), the overall benefits seem to be very small. Therefore, the widespread use of these agents cannot be recommended on the basis of the present evidence (Evidence D).

There is no evidence to support the use of heliox, DNase or mucolytics for the treatment of acute asthma in childhood.

UK, Feb 2009

British Guidelineon the Management of Asthma, 2008

Table 2Overview of the Evidence for Cold Therapies in Children

Therapy Study findingsCough (Cochrane review [seven studies])5; one RCT10Antihistamines Two studies: no benefit

Antihistamine/decongestant combination

Two studies: no benefit

Codeine plus guaifenesin (Robitussin AC)

One study: no benefit

Dextromethorphan (Delsym) Two studies: no benefitDextromethorphan plus guaifenesin

(Robitussin DM)One study: no benefit

Dextromethorphan plus salbutamol* One study: no benefitMucolytic (e.g., Letosteine*) One study: benefit

Other combinations One study: no benefitCongestion and rhinorrhea (Cochrane reviews [four studies]6)

Antihistamines Two studies (one using astemizole†): benefit

Antihistamine/decongestant combination

Two studies: no benefit

Decongestants No studies

2007 American Academy of Family Physicians.

AntihistaminesDrugs that directly

compete with

histamine for specific

receptor sites

Two histamine

receptors H1 (histamine1)

H2 (histamine2)

H1 histamine receptor- found on smooth muscle, endothelium, and central nervous system tissue; causes vasodilation, bronchoconstriction, smooth muscle activation, and separation of endothelia cellss (responsible for hives), and pain and itching due to insect stingsH1 antagonists are commonly referred to as antihistamines Antihistamines have several properties

Antihistaminic Anticholinergic Sedative

Antihistamines: IndicationsManagement of: Nasal allergies Seasonal or perennial allergic rhinitis

(hay fever) Allergic reactions Motion sickness Histamine-mediated disorders

Allergic rhinitis (hay fever, mould and dust allergies) Anaphylaxis Angioneurotic edema Drug fevers Insect bite reactions Urticaria (itching)

ACCP Cough guideline Patients with acute cough (as well as postnasal drip [PND]

and throat clearing) associated with the common cold can be treated with a first-generation antihistamine/decongestant (A/D) preparation (brompheniramine and sustained-release pseudoephedrine). Naproxen can also be administered to help decrease cough in this setting. Level of evidence, fair; benefit, substantial; grade of recommendation, A

In patients with the common cold, newer generation nonsedating antihistamines are ineffective for reducing cough and should not be used. Level of evidence, fair; benefit, none; grade of recommendation, D

Pratter MR. Cough and the common cold: ACCP evidence-based clinical practice guidelines. Chest 2006 Jan;129(1 Suppl):72S-4S.

Antihistamines

Ex: Diphenhydramine, chlorphenamine, brompheniramineMOA: H1 blocker; competes with receptor sites in resp.

tract, GI, blood vesselsAdv eff:

CNS drowsiness, headache, fatigue, nervousness, dizziness Anticholinergic (drying) effects, most common

Dry mouth Difficulty urinating Constipation Changes in vision

Arrhythmia, hallucinations, heart block, paradoxic excitability, respiratory depression, sedation, tachycardia,

GIT: appetite increase, weight gain, diarrhea, n/v Arthralgia, pharyngitis

Antihistamines:

Contraindicated in the presence of acute asthma attacks and lower respiratory diseases

Use with caution in increased intraocular pressure, cardiac or renal disease, hypertension, asthma, COPD, peptic ulcer disease, BPH, or pregnancy

Nonsedating/Peripherally Acting Antihistamines Developed to eliminate unwanted side

effects, mainly sedation Work peripherally to block the actions of

histamine; thus, fewer CNS side effects Longer duration of action (increases

compliance) Examples: cetirizine (virlix),

fexofenadine(allegra)

ACCP Evidence-based Clinical Practice Guidelines,

1. In patients with the common cold, newer generation nonsedating antihistamines are ineffective for reducing cough and should not be used. Level of evidence, fair; benefit, none; grade of recommendation, D

Pratter MR. Cough and the common cold: ACCP evidence-based clinical practice guidelines. Chest 2006 Jan;129(1 Suppl):72S-4S.

DECONGESTANTS

Oral Decongestants Prolonged decongestant

effects, but delayed onset

Effect less potent than topical

No rebound congestion MOA: Exclusively

adrenergics Example:

pseudoephedrine, Sinutab, Dristan, Tylenol cold, Sudafed

Adverse effect:agitation, anorexia, dysrhythmia, dystonic reactions, headache, hypertension, irritability, nausea, palpitations, seizure, sleeplessness, tachycardia, vomiting

Phenylpropanolamine has been associated with an increased risk of hemorrhagic stroke (bleeding into the brain or into tissue surrounding the brain) in women. Men may also be at risk. Although the risk of hemorrhagic stroke is low, the U.S. Food and Drug Administration (FDA) recommends restricted use of phenylpropanolamine.

Topical Nasal DecongestantsMOA: Adrenergics

Constrict small blood vessels that supply URI structures

As a result these tissues shrink, and nasal secretions in the swollen mucous membranes are better able to drain

Topical adrenergics Prompt onset Potent Sustained use over several days causes rebound congestion,

making the condition worse

COMPOSITION:Each 1 mL of solution contains:        Phenylephrine HCl        5 mg        Pheniramine Maleate        2 mg

Nasal Decongestants: Decongestants may cause

hypertension, palpitations, and CNS stimulation

Repeated use of nasal decongestants causes a decreased sensitivity to their vasoconstrictor effect and a rebound phenomenon with increased nasal congestion and discharge.

Clients on medication therapy for hypertension should check with their physician before taking OTC decongestants

Assess for drug allergies

Topical Nasal Decongestants (cont’d) Intranasal steroids

beclomethasone dipropionate flunisolide fluticasone

MUCOLYTICS

MucolyticsACETYLCYSTEINE

MOA: free sulfhydryl grp opens up disulfide bonds in mucoproteins

= ↓ viscosityAdv rxns: GI n/v; unpleasant odor

CNS: drowsiness, chillsResp: bronchospasm, rhinorrhea, hemoptysislocal irritation, clamminess, rash

Dose: 1 sachet through inh.

MucolyticAmbroxol MOA: breakdown of acid mucopolysaccharide fibers;

stimulates synthesis and release of surfactant by type II pneumocytes; stimulates the ciliary activity thereby improving mucokinesis (transport of mucous), Ambroxol is a metabolite of bromhexine

Adv effects: allergic responses such as skin eruption, urticaria or engioneurotic edema may occur. While used for a long time, epigastric pain, nausea and dizziness may occur.

EXPECTORANTS

Expectorants:

Reflex stimulation Agent causes irritation of the GI tract Loosening and thinning of respiratory tract

secretions occur in response to this irritationExample: guaifenesin

Direct stimulation The secretory glands are stimulated directly to

increase their production of respiratory tract fluidsExamples: iodine-containing products such as

iodinated glycerol and potassium iodide

COUGH AND COLD PREPARATIONSExpectorants

GUAIFENESINMOA: stimulates resp tract secretions = ↑ secretions ↓ viscosityAdv rxns: GI n/v, stomach painsCNS drowsiness, headachesRashesDose:100 mg q 4-6

ANTITUSSIVES

COUGH AND COLD PREPARATIONSANTITUSSIVES: OPIOIDS

CODEINE

MOA:: central; depression of medullary centerbinds to opiate receptors in the CNS, = altered perception & response to painAnalgesic / Narcotic / Antitussive

Adv effectsCNS: drowsiness, dizziness, light-

headedness, malaise, headache,restlessness CNS depression

Resp: shortness of breath, dyspneaCVS: tachycardia or bradycardia, hypotensionGIT: anorexia, nausea, vomitingHepatic: altered liver enzymes (ALT, AST)gut: decreased iromatopm. Iretera; spasmDerma: rash, urticaria, burning at IV site

Dose: 30 mg q 6-8h; SR 60 mg BID max 120 mg/day

COUGH AND COLD DRUGSANTITUSSIVES

DEXTROMETHORPHAN (DM)MOA: central: depresses medullary center but

lacking narcotic properties exc in overdose• Suppress the cough reflex by numbing the stretch receptors in the respiratory tract and preventing the cough reflex from being stimulated

Adv reactionsCNS: drowsiness, dizziness, comaResp depressionGIT: n/v, constipation, abdominal discomfort

Dose: 10-20mg q 4 or 30 mg q 6-8

OTC Restrictions for cough and cold preparations Medicine and Healthcare products Regulatory Agency in the UK

has banned the sale of over the counter cough and cold medicines for babies and young children under the age of 2 as a precautionary measure against accidental overdose because of an increase in reports of adverse reactions linked to overdose.

The cough and cold medicines which will no longer be licensed for children under the age of 2 years, contain the ingredients: brompheniramine, chlorphenamine & diphenhydramine (antihistamines); dextromethorphan and pholcodine (antitussives); guaifenesin and ipecacuanha (expectorants); phenylephrine, pseudoephedrine, ephedrine, oxymetazoline and xylometazoline

(decongestants).Royal Pharm Society Great Brit, Mar 2009

OTC cough and cold restrictions Health Canada has advised the public that certain over-the-counter cough

and cold medicines should not be used in children under 6 yearsof age, following a review of additional data. The Agency also says that cough and cold medicines marketed for use in children will require enhanced labelling and packaging and that it is working withmanufacturers to revise the labelling of these products.

New Zealand(2). In December 2007, the Medicines Adverse Reactions Committee (MARC) reviewed the safety and efficacy of cough and coldmedicines in children and recommended that these products should becontraindicated in children under two years of age, based on limited evidence for efficacy in this age group, an absence of evidence-based dosing, and evidence of significant toxicity in overdose.

The affected products are those containing bromhexine, brompheniramine,chlorpheniramine, dextromethorphan, diphenhydramine, doxylamine,guaifenesin, ipecacuanha, oxymetazoline, phenylephrine, pholcodine, promethazine, pseudoephedrine, triprolidine and xylometazoline.

No.2, 2009

COUGH AND COLD PREPARATIONS

COMBINATION PREPARATIONSColvan: DM + Guaifenesin + Chlorpheniramine + paracetamol

Dynatussin DM + Guaifenesin + Phenylpropanolamine + Na citrate

Tuseran DM + phenylpropanolamine + guiafenesin

Eurocof Guaiafenesin + chlorpheniramine + Na citrate

http://advantacell.com/redirect?url=aHR0cDovL3VwbG9hZC53aWtpbWVkaWEub3JnL3dpa2lwZWRpYS9jb21tb25zLzYvNmQvQ0RDX0dldF9TbWFydF9wb3N0ZXJfaGVhbHRoeV9hZHVsdC5wbmc%3D

ACCP cough guideline In patients with cough and acute upper respiratory tract

infection (URTI), because symptoms, signs, and even sinus imaging abnormalities may be indistinguishable from acute bacterial sinusitis, the diagnosis of bacterial sinusitis should not be made during the first week of symptoms. (Clinical judgment is required to decide whether to institute antibiotic therapy.) Level of evidence, fair; benefit, none; grade of recommendation, D

Pratter MR. Cough and the common cold: ACCP evidence-based clinical practice guidelines. Chest 2006 Jan;129(1 Suppl):72S-4S.

32

Management of Stable COPD

Other Pharmacologic Treatments

Antibiotics: Only used to treat infectious exacerbations of COPD

Antioxidant agents: No effect of n-acetylcysteine on frequency of exacerbations, except in patients not treated with inhaled glucocorticosteroids

Mucolytic agents, Antitussives, Vasodilators: Not recommended in stable COPD

The art of medicine consists of amusing the patient while nature cures the disease. - Voltaire