DROGAS

ANTITUSIGENAS
MUCOLITICAS Y
EXPECTORANTES
(mucoquineticos)
TOS = MECANISMO DE DEFENSA
* Receptores xa
la irritacin
*Pleura
*Diafragma
*Vas respiratorias
N vago (X)
Centro tusgeno
Reg lateral de medula
Oblonga y region pontina
Cierran la glotis y
contraen el diafragma
Musc Intercostales y
abdominales
Sntoma molestoso
Narcticos: Deriv Opio: morfina y
herona. Hidrocodona.
+G fenantreno: codena.
No narcticos: G morfinano: Dxmetorfano,
clobutinol, folcodina.
Antitusgenos de accin central
( umbral xa el reflejo de la tos en c. de la tos o depresin
sensibilidad).
Antitusgenos de accin
perifrica (bloquean a los R perifericos)
- Anestsicos locales: lidocaina, tetracaina
y cocaina. Benzonatato
- Broncodilatadores: metilxantinas y B2-
adrenergicos.
- Antihistamnicos: clorfedianol.
- Expectorantes o Mucokineticos.
* Liberacin de
histamina =
broncoespasmo
DERIVADOS DEL OPIO
(analgsicos)
G. Fenantrenico:
morfina y codena
G. Benzilisoquinolonicos:
Papaverina y noscapina.
*
Depresores
del centro
respiratorio
- Tos grave y persistente
- Producen adiccin y depresin.
MORFINA Y
HERONA
ANTITUSGENOS DE ACCION CENTRAL:
NARCTICOS
CODEINA
Metil ter de morfina
Alivia el dolor. Analgsico 65 mg = 650 mg de ASA y
acetaminofen. Antitusigeno o parte.
Disminuye el reflejo tusgeno central.
VENTAJAS VS. MORFINA
- Mejor tolerancia
- Menor adiccin y euforia
- Bajo riesgo de broncoespasmo
- Moderado fecto constipante y
emtico.
- VO, poco riesgo de sobredosis.
FARMACOCINTICA
-Concentracin mx
en plasma de 1 h
- T : 3.5 h
- Elimina orina
- 10% es desmetilada a
morfina.
- Absorcin rpida
por v. oral
-Metaboliza enHgado x
glucoronoconjugacion
CODEINA
FARMACOPATOLOG
A
Mareo
Somnolencia
Constipacin
Sequedad de boca
Viscosidad de secreciones
bronquiales
Dosis = depresin Respiratoria.
Tx NALOXONA
Hiperhidrosis, Agitacin
n-v
CODEINA
+ potente que
codena y
< Constipacin, pero
> Riesgo adiccin.
ANTITUSIGENOS NO
NARCOTICOS
Derivados del morfinano (poca accin sedante y
analgsica). Dxmetorfano, Clobutinol, folcodina.
En general, no producen adiccin.
DEXTROMETORFAN
O
Dextro isomero del narctico
morfinano.
Potencia = codeina
Umbral de percepcin a
estmulos tusgenos.
Frmacopatologa: NAUSEA,
MAREO. Dosis : depresin SNC
y efectos causados por liberacin de
histamina.
CLORFEDIANOL
(antihistaminico)
Estructuralmente parecido a difenhidramina
(benadryl)
EFECTOS: antihistaminicos, anticolinergicos y
leve anastesicos.
Dosis terapeuticas: sedacion
Dosis : excitacin central con irritabilidad y
alucinaciones.
VENTAJA?: accin duradera y estimular c
respiratorio.
- Potencia leve a moderada
- NO Hbito
- NO depresin del centro respiratorio
-Nausea
- Sueo
- Su efecto NO es mediado por R opiaceos
- No se metaboliza a morfina = NO efecto narctico
- NO adiccin
- NO deprime la respiracin y SNC .
Accin 12 h
(silomat)
NO NARCOTICOS
- Anestsicos locales.
- Broncodilatadores
- Mucoliticos-Mucokineticos.
- Antihistamnicos.
ANESTSICOS LOCALES
PARA SEDAR LA TOS EN
PROCEDIMIENTOS:
Endoscpicos (broncoscopa) o
Diagnsticos (broncografa)
-Se instalan en las
vas respiratorias
anestsicos tpicos
( cocana o tetracana)
-Efectos tpicos e
infiltrativos (lidocana)
PARA SEDAR LA TOS EN
PRESENCIA DE:
Cuerpo extrao en las vas
respiratorias
Tos severa en el asma
Micronebulizacin de
lidocana 0.5-1.0 %
(broncodilatador)
Lidocaina, Cocana o tetracaina
Son otros medicamentos que pueden
disminuir la tos por tener ligera
accin anestsica local
Oxolamine
Difenhidramina
Carafen
Relacionado con
la tetracana
La sobredosis
estimula el
S.N.C
La sobredosis
produce
convulsiones o
coma
Accin central
antitusgena NO
DEPRIME EL
CENTRO
RESPIRATORIO
Disminuye los
I.V.A de los
receptores de
la tos
(Acido butilaminobenzoico)
Cefalea, mareos
Tiene mal sabor
y produce
anestesia bucal.
Produce molestias
G-I
Rash cutneo
con prurito
BENZONATATO. EFECTOS ADVERSOS
BRONCO DILATADORES
Metilxantinas y
Estimulantes B2-adrenergicos
Al el espasmo bronquial calman la tos
EXPECTORANTES
(mucoquineticos)
1. INHALACION: ClNa, ClNa
hipertonico1.8-20% y propilenglicol.
2. VO: Acetilcisteina, Guayacolato de
glicerilo o guayfenesina, Ipecacuana,
Yoduro de K, Bromhexina,
carboximetilcisteina, Ambroxol.
EXPECTORANTES (mucoquineticos)
Inhalacin
Cl Na Cl Na hipertnica
1.8 - 20%
aerosol
Propilenglicol
Nausea, vomito, Broncoespasmo,
irritacin de mucosa bucal y faringeas
PROPILENGLICOL
Propiedades higroscopicas, se
disuelve en H20, sabor dulce,
no irritante.
humectante y demulcente.
Soluciones 2-5% en fibrosis
qustica de pncreas.
15-20% con solucin salina
hipertnica para inducir
esputo.
(inhaloterapia)
Acetil Cisteina
MEC ACCION:
Rompe los puentes de unin
de disulfuro de las
mucoprotenas. Liquificar.
viscosidad del esputo, no
rompe el DNA.
No accin sobre fibrina o
cogulos sanguneos
Se usa por instilacin directa
al rbol bronquial.
No se debera usar por
inhalacin y NO es efectiva
por VO.
Evita progresin de
enfisema
mucoltico
Expectorantes administrados por
va oral
Irritan la mucosa gstrica que
provoca un reflejo vagal
mucoquinetico gastro-pulmonar
aumentando la secrecin bronquial,
requiriendo dosis emticas.
-Guayacolato de glicerilo o guayfenesina
-Ipecacuana
-Ioduro de K, Cloruro de amonio y Citrato de Na
-Bromexina
-Carboximetilcisteina
-Ambroxol
Guayacolato de
Glicerilo:Guayfenesina
A dosis altas 2400mg diarios
til mucokineticos que por va
refleja (accion emetica)
produce broncorrea
Dosis empleadas es 800mg/d.
Placebo !!
Expectorante ???
IPECACUANA
Emtica, el extracto contiene
alcaloides emetina y cefalina
En dosis subemeticas es
estimulador del reflejo vagal
gastropulmonar mucokintico
Incremento de la secrecin de
glndulas bronquiales
Caphelis acuminata
Ioduro de Potasio
A largo plazo = bloque de la tiroides.
Estimula el reflejo vagal
gastropulmonar mucokinetico y
secrecin de glndulas bronquiales
Estimula el movimiento ciliar.
Estimula digestin del moco por las
enzimas proteolticas naturales.
FARMACOPATOLOGA: nausea,
vomito, rinorrea, eritema, acne,
urticaria, hipotiroidismo.
Expectorante a dosis terapeutica?
Cloruro de amonio
200mg a un gramo en
5ml.
Estimulando el reflejo
vagal gastro-pulmonar
Citrato de sodio
Subemetica por va
oral
nebulizaciones
Mucolytics
-Bromhexine
- Oral mucolytics; loosen and thin bronchial
secretions by reducing surface tension and
viscosity of mucus.
- Dizziness, headache, rash - these rarely
occur at therapeutic doses. Nausea/vomiting,
abdominal pain, diarrhoea
- expectoracin
- de viscosidad. (H2O y
despolimerizacion de mucopolisacaridos).
Obtenido de la planta Adhatoda basica
Origen India (tos y asma)
BROMEXINA
CARBOXIMETILCISTEINA
VO. (Acetilcisteina uso solo x local o
inhalacion).
viscosidad del esputo rompiendo
los puentes sulfhidrilos que unen
los mucopolisacridos.
AMBROXOL
- Broncosecretolitico.
- Estimulante del Surfactante
- la viscosidad del esputo
- Antioxidante
- Antiinflamatorio x interferencia con
Ac araquidonico.
Cough and cold remedies for children
Valerie Sung, University of Melbourn
Key words: children, over-the-counter medicines.
(Aust Prescr 2009; 32:122-4)
Summary
Over-the-counter cough and cold remedies for children under 2 years of
age have recently been rescheduled to prescription-only. This will mean
that doctors and pharmacists will encounter more consultations for such
medicines.
These drugs are no longer recommended in children because of the lack
of efficacy and reports of serious adverse events.
Cough and cold remedies for children
Valerie Sung, University of Melbourn
Key words: children, over-the-counter medicines.
(Aust Prescr 2009; 32:122-4)
Summary
Over-the-counter cough and cold remedies for children under 2 years of age have recently been rescheduled to prescription-only.
This will mean that doctors and pharmacists will encounter more consultations for such medicines. These drugs are no longer
recommended in children because of the lack of efficacy and reports of serious adverse events.
Introduction
Upper respiratory tract infections are common in children and it is not surprising that cough and cold symptoms can be a major
burden to many families. Until recently, over-the-counter (OTC) cough and cold remedies were widely available in Australia, and
extensively used in young children. They include antitussives, antihistamines, expectorants and decongestants (Table 1).
However, since September 2008 cough and cold medicines for children less than two years have been rescheduled to S4 to become
prescription-only. The USA and the UK introduced similar restrictions in response to reports of adverse effects, accidental
overdoses and lack of evidence of their efficacy for acute and chronic cough in children.
Cough in children
Cough is a reflex response to mechanical, inflammatory and chemical irritation of the tracheobronchial tree. It is a normal
mechanism for the maintenance of a healthy respiratory system.
Diagnosis
When a child presents with cough or cold symptoms, the most important first step is to make the correct diagnosis and exclude
serious pathology. Most causes of cough are self-limiting and do not require investigations. A detailed history and physical
examination are most important, followed by specific investigations only when clinically indicated.
Causes of cough
Management of a cough should be directed at the underlying cause. Cough that is accompanied by other upper respiratory tract
infection symptoms, such as rhinorrhoea and sore throat, is usually due to viral infections and is rarely bacterial. If such a cough
lingers, it may be a postinfective cough. A barking or brassy cough may suggest croup or tracheomalacia. Cough accompanied by
respiratory distress suggests pneumonia or bronchiolitis. Asthma may present as nocturnal cough, while cough that disappears
when the child is asleep may suggest a psychogenic cause.
A coughing infant or child with paroxysms of cough may have pertussis. Suppurative lung disease should be considered if the
cough is most vigorous in the morning. If there is a temporal association with feeding or with positioning, gastro-esophageal
reflux should be considered.
The presence of a foreign body should be suspected after an acute episode of choking, while aspiration may occur in children with
hypotonia or pharyngeal incoordination. Chlamydia trachomatis is an uncommon but serious cause of cough that should be
considered especially if the infant has conjunctivitis or whose mother has evidence of chlamydial infection. Structural anomalies
causing cough are usually associated with other symptoms such as stridor or cyanosis.
Symptomatic treatments for colds and cough
Cough and cold symptoms can cause significant distress to children and
their families, and this is reflected in the vast array of OTC medications
marketed over the years. Most cough and cold remedies are a combination
of antitussives, antihistamines, expectorants and decongestants.
Antitussives
Pholcodine Centrally acting opioid derivative; directly suppresses medullary cough centre
Dizziness, sedation, nausea Opioid dependence, potential abuse, serotonin syndrome,
lethargy, stupor, aspiration
Dextromethorphan Narcotic analogue; directly suppresses medullary cough centre
Antihistamines
Diphenhydramine Brompheniramine Chlorpheniramine Histamine H1-receptor antagonists;
prevent histamine-induced reactions in cells of the respiratory tract, gastrointestinal tract and
blood vessels Sedation, headache, dizziness, nervousness, restlessness, irritability, palpitations
Hallucinations, seizures, central nervous system depression, cardiovascular collapse, apnoea,
death, anticholinergic effects
Decongestants
Pseudoephedrine Phenylephrine Sympathomimetic drugs, adrenergic receptor agonists;
produce vasoconstriction within the respiratory tract mucosa, and cause increased heart rate
and cardiac contractility Nervousness, restlessness, insomnia, trembling, headache, anxiety
Tachycardia, palpitations, dysrhythmias, hypertension, hallucinations, agitation, central
nervous system depression, seizures
Expectorants
Guaifenesin Ipecacuanha Expectorants; promote the expulsion of mucus and other materials
from the respiratory tract Drowsiness, dizziness, headache, rash - these rarely occur at
therapeutic doses Nausea/vomiting, abdominal pain, nephrolithiasis