Lecture 10 Respiratory Drugs

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RESPIRATORY DRUGS

RESPIRATORY SYSTEM
RESPONSIBLE FOR MEDIATING GAS EXCHANGE
BETWEEN THE EXTERNAL ENVIRONMENT AND THE
BLOODSTREAM
THE UPPER RESPIRATORY TRACT CONDUCTS AIR TO
THE LOWER RESPIRATORY PASSAGES AND
ULTIMATELY TO THE LUNGS

RESPIRATORY SYSTEM
HUMIDIFIES AND CONDITIONS INSPIRED AIR AND SERVES
TO PROTECT THE LUNGS FROM HARMFUL SUBSTANCES
GAS EXCHANGE TAKES PLACE BETWEEN THE ALVEOLI
AND THE PULMONARY CIRCULATION
FUNCTION: MAINTAINING PROPER AIRFLOW THROUGH
THE RESPIRATORY PASSAGES

RESPIRATORY DRUGS
FIRST GROUP
INCLUDES DRUGS THAT TREAT ACUTE AND
RELATIVELY MINOR PROBLEMS
EX. NASAL CONGESTION, COUGHING, AND
SEASONAL ALLERGIES

RESPIRATORY DRUGS
SECOND GROUP
THE SECOND CATEGORY INCLUDES DRUGS THAT
TREAT MORE CHRONIC AND SERIOUS AIRWAY
OBSTRUCTIONS, EX. BRONCHIAL ASTHMA,
CHRONIC BRONCHITIS, AND EMPHYSEMA

RESPIRATORY THERAPY
PHYSICAL THERAPISTS AND OCCUPATIONAL
THERAPISTS WILL FREQUENTLY TREAT PATIENTS
WITH BOTH ACUTE AND CHRONIC RESPIRATORY
CONDITIONS

DRUGS USED TO TREAT AND CONTROL


RESPIRATORY TRACT IRRITATION AND
SECRETIONS
TREAT SYMPTOMATIC COUGHING AND IRRITATION
RESULTING FROM COMMON COLD, SEASONAL
ALLERGIES, AND UPPER RESPIRATORY TRACT
INFECTIONS
MANY OF THESE DRUGS ARE FOUND IN OVER-THECOUNTER PREPARATIONS

DRUGS USED TO TREAT AND CONTROL


RESPIRATORY TRACT IRRITATION AND
SECRETIONS
SEVERAL DIFFERENT AGENTS ARE COMBINED IN THE SAME
COMMERCIAL PREPARATION
EX. A DECONGESTANT, AN ANTITUSSIVE, AND AN EXPECTORANT MAY
BE COMBINED AND IDENTIFIED BY A SPECIFIC TRADE NAME.
AGENTS WITHIN A SPECIFIC CATEGORY MAY HAVE PROPERTIES THAT
OVERLAP INTO OTHER DRUG CATEGORIES
CERTAIN ANTIHISTAMINES MAY ALSO HAVE ANTITUSSIVE PROPERTIES

ANTITUSSIVES
USED TO SUPPRESS COUGHING ASSOCIATED WITH THE
COMMON COLD AND FLU SYMPTOMS
USUALLY RECOMMENDED FOR SHORT-TERM USE IN
RELIEVING SYMPTOMATIC COUGHING
THE EXTENSIVE USE OF ANTITUSSIVES HAS BEEN
QUESTIONED IN OUR SOCIETY

ANTITUSSIVES
COUGHING IS A DEFENSE MECHANISM THAT HELPS
EXPEL MUCUS AND FOREIGN MATERIAL FROM THE
UPPER RESPIRATORY TRACT
ANTITUSSIVES MAY REDUCE THE ABILITY OF COUGHING
ANTITUSSIVES MAY BE HELPFUL IN TREATING AN
ANNOYING DRY COUGH
USE OF THESE DRUGS TO TREAT AN ACTIVE AND
PRODUCTIVE COUGH MAY NOT BE JUSTIFIED

ANTITUSSIVES
THERE IS ALSO CONCERN THAT MANY ANTITUSSIVES
ARE NOT REALLY EFFECTIVE IN TREATING COUGH
OVER-THE-COUNTER PRODUCTS MAY NOT CONTAIN AN
ADEQUATE AMOUNT OF THE ACTIVE MEDICATION AND
MAY BE NO MORE EFFECTIVE THAN PLACEBO IN
TREATING COUGH
DOSES THAT ARE EFFECTIVE IN TREATING COUGH MAY
ALSO PRODUCE SERIOUS SIDE EFFECTS

ANTITUSSIVES
MECHANISM UNDER THE COUGH REFLEX CONTINUE TO
BE STUDIED SO THAT SAFER AND MORE EFFECTIVE
ANTITUSSIVES CAN BE DEVELOPED
CODEINE AND SIMILAR OPIATE DERIVATIVES SUPPRESS
THE COUGH REFLEX BY A CENTRAL INHIBITORY EFFECT

ANTITUSSIVES
NONOPIOID ANTITUSSIVES INHIBIT THE IRRITANT EFFECTS
OF HISTAMINE ON THE RESPIRATORY MUCOSA OR BY A
LOCAL ANESTHETIC ACTION ON THE RESPIRATORY
EPITHELIUM
THE PRIMARY ADVERSE EFFECT ASSOCIATED WITH MOST
ANTITUSSIVES IS SEDATION, DIZZINESS AND
GASTROINTESTINAL UPSET MAY ALSO OCCUR

COMMON ANTITUSSIVE AGENTS


GENERIC
MOA
NAME

TRADE NAME

BENZONATATE
ANESTHETIC EFFECT ON
CODEINE
COUGH REFLEX BY
CENTER

TESSALON

LOCAL
RESPIRATORY MUCOSA

MANY TRADE NAMES


DIRECT EFFECT ON BRAINSTEM

DEXTROMETHORPHAN
COUGH REFLEX (SIMILAR

MANY TRADE NAMES


TO CODEINE) BUT IS NON-

INHIBITS
COUGH
INHIBITS
NARCOTIC

COMMON ANTITUSSIVE AGENTS


GENERIC
MOA
NAME

DIPHENHYDRAMINE
ANTIHISTAMINE
HYDROCODONE
CODEINE
HYDROMORPHONE
CODEINE

TRADE NAME
BENADRYL
DONATUSSIN, HYDROPANE
TUSSIGON
ILAUDID

SIMILAR TO
SIMILAR TO

DECONGESTANTS
CONGESTION AND MUCOUS DISCHARGE FROM THE
UPPER RESPIRATORY TRACT ARE FAMILIAR SYMPTOMS
ALLERGIES, COMMON COLD, AND VARIOUS
RESPIRATORY INFECTIONS OFTEN PRODUCE A RUNNY
NOSE AND A STUFFY HEAD SENSATION

DECONGESTANTS
DECONGESTANTS USED TO TREAT THESE SYMPTOMS ARE
USUALLY ALPHA-1ADRENERGIC AGONISTS
THESE AGENTS BIND TO ALPHA-1 RECEPTORS LOCATED ON
THE BLOOD VESSELS OF THE NASAL MUCOSA AND STIMULATE
VASOCONSTRICTION
EFFECTIVELY DRY UP THE MUCOSAL VASCULATURE
DECREASING LOCAL CONGESTION IN THE NASAL PASSAGES

DECONGESTANTS
AGENTS TAKEN SYSTEMICALLY OR APPLIED LOCALLY TO
THE NASAL MUCOSA VIA AEROSOL SPRAYS
OCCASIONAL USE OF THESE DRUGS CAN HELP THE
SYMPTOMS RELATED TO NASAL CONGESTION

DECONGESTANTS
MIMIC THE EFFECTS OF INCREASED SYMPATHETIC
NERVOUS SYSTEM ACTIVITY AND CAN CAUSE SERIOUS
CARDIOVASCULAR AND CENTRAL NERVOUS SYSTEM
(CNS) EXCITATION
EXCESSIVE USE OR ABUSE SHOULD BE AVOIDED

DECONGESTANTS
PRIMARY ADVERSE EFFECTS ASSOCIATED ARE
HEADACHE, DIZZINESS, NERVOUSNESS, NAUSEA,
INCREASED BLOOD PRESSURE, PALPITATIONS
THESE EFFECTS BECOME MORE APPARENT AT HIGHER
DOSES AND DURING PROLONGED OR EXCESSIVE DRUG
USE

COMMON DECONGESTANTS
GENERIC NAME
DOSAGE FORMS
EPHEDRINE
OXYMETAZOLINE
NASAL SPRAY

TRADE NAME
RYNATUSS
AFRIN, DRISTAN
12-HR NASAL SPRAY

PHENYLEPHRINE
NASAL SPRAY

NEO-SYNEPHRINE

ORAL

COMMON DECONGESTANTS
GENERIC NAME
DOSAGE FORMS

TRADE NAME

PSEUDOEPHEDRINE
ORAL

DIMETAPP

DECONGESTANT, SUDAFED
XYLOMETAZOLINE
SPRAY

OTRIVIN

NASAL

ANTIHISTAMINES
USED FOR SEDATION; TREATMENT OF PARKINSONISM
TREATMENT OF THE RESPIRATORY ALLERGIC RESPONSE
TO SEASONAL ALLERGIES (HAY FEVER, AND SO FORTH)
AND OTHER ALLERGENS
ARE ENDOGENOUS CHEMICALS THAT REGULATES
GASTRIC SECRETION, CNS NEURAL MODULATION AND
HYPERSENSITIVITY

ANTIHISTAMINES
EXERT ITS EFFECTS THROUGH 4 PRIMARY RECEPTOR
SUBTYPES:
H1, H2, H3, AND H4
SPECIFICALLY BLOCK THE H1 SUBTYPE OF HISTAMINE
RECEPTORS
THE EFFECTS OF HISTAMINE DURING ALLERGIC
REACTIONS, RESPIRATORY INFECTIONS ARE MEDIATED
THROUGH THE H1 RECEPTOR LOCATED ON VASCULAR,

ANTIHISTAMINES
DRUGS THAT SELECTIVELY BLOCK THE H2 RECEPTOR
(REFERRED TO AS H2 ANTAGONISTS) MAY HELP
CONTROL GASTRIC SECRETION IN CONDITIONS SUCH
AS PEPTIC ULCER
THE H3 RECEPTOR IS INVOLVED IN THE LOCAL
REGULATION OF HISTAMINE RELEASE FROM CNS NERVE
TERMINALS
H4 RECEPTOR HAS BEEN IDENTIFIED ON BLOOD CELLS

ANTIHISTAMINES
THE CLINICAL AND PHARMACOLOGIC SIGNIFICANCE OF H3
AND H4 RECEPTORS REMAINS TO BE DETERMINED
IT DECREASES NASAL CONGESTION BY BLOCKING THE
EFFECTS OF HISTAMINE ON THE UPPER RESPIRATORY
TISSUES, MUCOSAL IRRITATION AND DISCHARGE (RHINITIS,
SINUSITIS), AND CONJUNCTIVITIS CAUSED BY INHALED
ALLERGENS

ANTIHISTAMINES
DECREASE THE COUGHING AND SNEEZING
ASSOCIATED WITH THE COMMON COLD
ANTIHISTAMINES MAY BE USED AS AN ADJUNCT IN
PATIENTS WITH ASTHMA TO HELP CONTROL RHINITIS
AND SINUSITIS BUT DO NOT REVERSE BRONCHOSPASM

ANTIHISTAMINE SIDE EFFECTS


PRIMARY ADVERSE EFFECTS ARE SEDATION, FATIGUE,
DIZZINESS, BLURRED VISION, AND INCOORDINATION.
GASTROINTESTINAL DISTRESS (NAUSEA, VOMITING)
CERTAIN SIDE EFFECTS ARE RELATED DIRECTLY TO
EACH DRUGS ABILITY TO CROSS THE BLOOD-BRAIN
BARRIER

ANTIHISTAMINE SIDE EFFECTS


FIRST-GENERATION ANTIHISTAMINES READILY CROSS
THE BLOOD-BRAIN BARRIER AND ENTER THE BRAIN
CAUSING AS SEDATION AND PSYCHOMOTOR SLOWING
NEWER SECOND-GENERATION ANTIHISTAMINES DO
NOT EASILY CROSS THE BLOOD BRAIN BARRIER,
HENCE, SEDATION AND OTHER CNS SIDE EFFECTS IS
REDUCED SUBSTANTIALLY

ANTIHISTAMINE SIDE EFFECTS


NEWER AGENTS, ALSO KNOWN AS NONSEDATING
ANTIHISTAMINES, INCLUDE CETIRIZINE (ZYRTEC), LORATADINE
(CLARITIN), DESLORATIDINE (CLARINEX), AND FEXOFENADINE
(ALLEGRA
NEWER ANTIHISTAMINES ARE MORE SELECTIVE FOR THE H1
RECEPTOR SUBTYPE AND PRODUCE FEWER SIDE EFFECTS
RELATED TO OTHER HISTAMINE RECEPTORS

ANTIHISTAMINE SIDE EFFECTS


ASTEMIZOLE AND TERFENADINE MAY BE CARDIOTOXIC, AND
PROBLEMS SUCH AS SEVERE VENTRICULAR ARRHYTHMIAS
(TORSADES DE POINTES)
NON-SEDATING AGENTS HAVE BECOME THE AGENTS OF CHOICE
FOR MANY PEOPLE BECAUSE THEY DECREASE HISTAMINERELATED SYMPTOMS WITHOUT PRODUCING EXCESSIVE SEDATION
AND OTHER NEUROPSYCHIATRIC EFFECTS

ANTIHISTAMINES
GENERIC NAME
POTENTIAL
AZATADINE
BROMPHENIRAMINE
CARBINOXAMINE
MODERATE

TRADE NAME

SEDATION

OPTIMINE

LOW

BROMPHEN,DIMETAPP
RONDEC

CETIRIZINE
LOW

ZYRTEC

CHLORPHENIRAMINE

CHLOR-TRIMETON

LOW

LOW TO
VERY
LOW

ANTIHISTAMINES
GENERIC NAME
POTENTIAL
CLEMASTINE
CYPROHEPTADINE
DESLORATIDINE
LOW

TRADE NAME
TAVIST
PERIACTIN
CLARINEX, AERIUS

SEDATION
LOW
MODERATE
VERY

DEXCHLORPHENIRAMINE POLARAMINE

LOW

DIMENHYDRINATE

HIGH

DRAMAMINE

ANTIHISTAMINES
GENERIC NAME
POTENTIAL

TRADE NAME

DIPHENHYDRAMINE

BENADRYL

DOXYLAMINE
SLEEP-AID

UNISOM

FEXOFENADINE
ALLEGRA
LOW
HYDROXYZINE
MODERATE LORATADINE
VERY LOW

SEDATION
HIGH
HIGH
VERY
ATARAX
CLARITIN

ANTIHISTAMINES
GENERIC NAME
POTENTIAL

TRADE NAME

PNINDAMIN

NOLAHIST

PYRILAMINE
MODERATE

CODIMAL

TRIPELENNAMINE
MODERATE
TRIPROLIDINE

SEDATION
LOW

PBZ
ACTIFED

LOW

MUCOLYTICS AND EXPECTORANTS


MUCOLYTIC DRUGS ATTEMPT TO DECREASE THE VISCOSITY OF
RESPIRATORY SECRETIONS
EXPECTORANT DRUGS FACILITATE THE PRODUCTION AND
EJECTION OF MUCUS
THESE DRUGS ARE USED TO PREVENT THE ACCUMULATION OF
THICK VISCOUS SECRETIONS THAT CAN CLOG RESPIRATORY
PASSAGES AND LEAD TO PULMONARY PROBLEMS

MUCOLYTICS AND EXPECTORANTS


EXPECTORANTS AND MUCOLYTICS ARE USED IN ACUTE
DISORDERS RANGING FROM THE COMMON COLD TO
PNEUMONIA, AS WELL AS IN CHRONIC DISORDERS SUCH AS
EMPHYSEMA AND CHRONIC BRONCHITIS
THESE DRUGS ARE OFTEN USED IN COMBINATION WITH OTHER
AGENTS (ANTITUSSIVES, DECONGESTANTS, BRONCHODILATORS)
SOME STUDIES HAVE DOCUMENTED THAT THESE DRUGS CAN
IMPROVE THE ABILITY TO EXPEL MUCUS AND INCREASE
PULMONARY FUNCTION

MUCOLYTIC
THE PRIMARY MUCOLYTIC DRUG CURRENTLY IN USE IS ACETYLCYSTEINE
THIS DRUG IS THOUGHT TO WORK BY SPLITTING THE DISULFIDE
BONDS OF RESPIRATORY MUCOPROTEINS FORMING A LESS VISCOUS
SECRETION
ACETYLCYSTEINE ALSO HAS ANTIOXIDANT EFFECTS, AND SOME OF
ACETYLCYSTEINES BENEFITS MAY BE DUE TO ITS ABILITY TO
DECREASE FREE-RADICAL DAMAGE IN THE RESPIRATORY TISSUES

MUCOLYTIC
ACETYLCYSTEINE IS USUALLY ADMINISTERED DIRECTLY
TO THE RESPIRATORY MUCOSA BY INHALATION OR
INTRATRACHEAL INSTILLATION (THROUGH A
TRACHEOSTOMY)
THE PRIMARY ADVERSE EFFECTS ASSOCIATED WITH
THIS DRUG INCLUDE NAUSEA, VOMITING,
INFLAMMATION OF THE ORAL MUCOSA (STOMATITIS),
AND RHINORRHEA

EXPECTORANT
BUT GUAIFENESIN IS THE ONLY DRUG CURRENTLY
ACKNOWLEDGED BY THE FDA TO HAVE EVIDENCE OF
THERAPEUTIC EFFECTS
THIS DRUG IS ADMINISTERED TO INCREASE THE
PRODUCTION OF RESPIRATORY SECRETIONS
ENCOURAGING EJECTION OF PHLEGM AND SPUTUM

EXPECTORANT
GUAIFENESIN, WHICH IS USUALLY ADMINISTERED ORALLY IN SOME
FORM OF SYRUP OR ELIXIR OFTEN COMBINED WITH OTHER AGENTS IN
OVER-THE-COUNTER PREPARATIONS
EXACT MECHANISM OF ACTION IS NOT FULLY UNDERSTOOD
PRIMARY ADVERSE EFFECT ASSOCIATED WITH GUAIFENESIN IS
GASTROINTESTINAL UPSET, WHICH IS EXACERBATED IF EXCESSIVE
DOSES ARE TAKEN OR IF THIS DRUG IS TAKEN ON AN EMPTY STOMACH

TAPOSNAPO!!!

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