Les antalgiques

 Les antalgiques


I. Définition

II. Les différentes classes d'antalgiques

1°/ Les antalgiques périphériques

a) Les AINS (Anti-Inflammatoires Non Stéroïdiens)
b)Les non morphiniques

2°/ Les antalgiques centraux faibles

a) La codéine
b) Le dextropropoxyphène
c) Le tramadol

3°/ Les antalgiques centraux puissants

a) Introduction
b) Principes d'utilisation

III. Traitements co-analgésiques

1°/ Les antidépresseurs

2°/ Les anti-spasmodiques

3°/ Les myorelaxants


I. Définition

Se dit d'un médicament utilisé dans la lutte contre la douleur. Il existe  plusieurs sortes d'antalgiques qui sont dispensés en fonction du type de douleurs rencontrées.

Ainsi l 'OMS (Organisation Mondiale de la Santé) a classé ceux-ci en trois paliers :

  • Palier I : Antalgiques périphériques (pour les douleurs légères à moyennes)

  • Palier II : Antalgiques centraux faibles (pour les douleurs moyennes à intenses)

  • Palier III : Antalgiques centraux forts ( pour les douleurs très intenses voire rebelles) 

 

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II. Les différentes classes d'antalgiques

Chaque antalgique sera détaillé de façon précise sous forme de tableau, exploitant pour tous la famille, les noms commerciaux, les actions, les contre-indications, les effets secondaires.

1°/ Les antalgiques périphériques (palier I)

On peut les qualifier d'usuels car ils sont ceux que chaque foyer garde dans sa pharmacie. En effet , ils sont utilisés dans le traitement des douleurs légères à moyennes. Plusieurs familles de médicaments sont utilisés comme antalgiques périphériques, les AINS ( Anti Inflammatoires Non Stéroïdiens) en font partie :

a) Les AINS

Ils sont utilisés soit en complément d'un traitement antalgique simple soit seul car ils ont une action anti-inflammatoire et anti pyrétique associées.

FAMILLE

NOM

ACTION

CONTRE INDICATION

EFFETS SECONDAIRES

Les Salycilés

Aspégic

Upsa

Catalgine

Solupsan

antalgique

antipyrétique

anti-inflammatoire

anti-agrégant plaquettaire

inhibition de l'acide urique

ulcère

traitement AVK

métrorragie

allergie

grossesse

troubles digestifs

syndrome hémorragique

allergie

insuffisance hépatique

baisse de l'acuité visuelle

céphalées

bourdonnement d'oreille

Les Pyrazolés

Butazolidine

anti-inflammatoire

anti-pyrétique

antalgiques

gastrite

déshydratation

traitements diurétiques

hypertension artérielle

asthme

sujets âgés

Digestif : nausées, douleurs abdominales, diarrhée, ulcération gastrique, hémorragie digestive

Rénale : insuffisance rénale fonctionnelle, syndrome néphrotique, rétention hydrosodée, hyponatrémie, hypokaliémie, élévation de la tension artérielle

Respiratoire : bronchospasme

Neurologie: vertiges, céphalées, surdité

Cutanée : allergie prurigineuse, érythème

Hématologie : anémie, agranulocytose, thrombopénie

Hépatique : hausse des transaminases, hépatite réactionnelle

Grossesse : allongement du temps de travail

Les Indoliques

Indocid

Arthrocid

Les Arylcarboxyliques

Voltarène

Profénid

Apranax

Nurofen

Brufen

Les Fénamates

Nifluril

Les Oxicams

Feldène

Cycladol

Tilcotil

b)Les non morphiniques

Ce sont les traitements antalgiques simples souvent couplés à une action anti-pyrétique

FAMILLE

NOM

ACTION

CONTRE INDICATION

EFFETS SECONDAIRES

Acide acétylsalicylique

Aspégic

Catalgine

antalgique

antipyrétique

ulcère

grossesse

allergie

traitement AVK

métrorragie

troubles digestifs

syndrome hémorragique

allergie

insuffisance hépatique

céphalées

acouphènes

baisse de l'acuité visuelle

Paracétamol

Dafalgan

Doliprane

Efféralgan

antalgique

antipyrétique

allergie

hépatopathie

alcoolisme

dénutrition

insuffisance rénale

érythème

urticaire

hépatites rares

thrombopénie rare

Noramidopyrine

Novalgine

Pyréthane

antalgique

< 15 ans

hypersensibilité aux pyrazolés ou aux salicylés

antécédents d'agranulocytose

porphyrie hépatique

Hématologie : agranulocytose, thrombopénie

Rénal : insuffisance rénale aiguë, néphropathie interstitielle

Cutané : urticaire, dermatose

Respiratoire : asthme

Coloration brunâtre des urines

NB : Surdosage au paracétamol

Le surdosage en paracétamol arrive trop fréquemment car ce médicament est en vente libre et un des produits les plus utilisé dans l'automédication, or une personne non informée sur la dose journalière à prendre risque d'être confrontée dans les premières 24 heures aux signes suivants en cas d'excès:

  • nausées, vomissements

  • anorexie

  • pâleur

  • douleurs abdominales

  • risque de cytolyse hépatique plus ou moins importante selon la quantité absorbée ( risque augmenté >10 g)

Antidote: Fluimicil ( mucolytique)

2°/ Les antalgiques centraux faibles (palier II)

Ces antalgiques opiacés faibles sont souvent associés à d'autres substances .Sur le marché nous trouvons rarement de la codéine ou du dextropropoxyphène pur, leur action est souvent couplée à celle d'un antalgique périphérique.

a) La codéine

FAMILLE

NOM

ACTION

CONTRE INDICATION

EFFETS SECONDAIRES

Codéine seule

Dicodin

Antalgique

hypothyroïdie

allergie

insuffisance respiratoire

asthme

< 15 ans

insuffisance hépatocellulaire et/ou rénale grave

Digestif : constipation, nausées, vomissements

Respiratoire : bronchospasme, dépression respiratoire

Neurologie : somnolence, vertiges

Cutané : allergie

> dose normale: risque de dépendance et de syndrome de sevrage

Codéine + paracétamol

Efféralgan codéiné

Codoliprane

Lindilane

Antalgique

Anti-pyrétique

< 15 ans

allergie

insuffisance respiratoire

asthme

idem Codéine seule + urticaire, thrombopénie rare

NB : Surdosage à la codéine

Il est possible chez les toxicomanes et autres que les doses normales soient largement dépassées .Ainsi des signes de surdosage apparaissent entraînant des conséquences plus ou moins graves.

Adulte :

dépression aiguë des centres respiratoires, oedème pulmonaire

Somnolence, ataxie

Rash cutané, prurit

Enfant :

Bradypnée

Myosis

convulsions

Visage bouffi, urticaire

Rétention urinaire

Collapsus

b)   Le Dextropropoxyphène

FAMILLE

NOM

ACTION

CONTRE INDICATION

EFFETS SECONDAIRES

Dextropropoxyphène seul

Antalvic

Antalgique

allergie

insuffisance rénale sévère

< 15 ans

Digestif : nausées, vomissements, douleur abdominales, constipation

Neuropsy : Céphalées, asthénie, euphorie, vertiges, somnolence, désorientation

Troubles visuels

Hypoglycémie

Allergie cutanée

Dextropropoxyphène + paracétamol

Di-Antalvic

Antalgique

Anti-pyrétique

c) Le Tramadol

FAMILLE

NOM

ACTION

CONTRE INDICATION

EFFETS SECONDAIRES

Tramadol

Topalgic

Prodalgic

Antalgique

Anti-inflammatoire faible

allergie au tramadol ou aux opiacés

intoxication aiguë ou surdosage avec des produits dépresseurs respiratoires du système nerveux central

traitement IMAO

insuffisance respiratoire sévère

insuffisance hépatocellulaire grave

< 15 ans

épilepsie non traitée

allaitement et grossesse

urticaire, oedème de Quincke

bronchospasme

convulsions

nausées, vomissement

céphalées, somnolence, vertiges

sécheresse buccale, hypersudation, constipation

rarement: douleurs abdominales, rash, euphorie, troubles mineurs de la vision

NB : Surdosage au  tramadol

Signes :

myosis, vomissements,

collapsus cardio-vasculaire

dépression respiratoire voire arrêt

coma, convulsions

3°/ Les antalgiques centraux puissants (palier III)

a) Introduction:

Le Pavot est un produit datant de l'antiquité où il était utilisé pour ses vertus calmantes. De cette plante a été extrait l'opium qui est en fait la substance au pouvoir analgésique grâce  à la morphine, son principale alcaloïde. D'autres substances aujourd'hui reproduisent les effets de la morphine, on les appelle les substances opioïdes.

La morphine est un antalgique à effet central. Son effet est dû à son action d'activation dite agoniste des récepteurs opioïdes qui sont les récepteurs µ (mu), delta, kappa , qui se situent au niveau de la moelle épinière et au niveau supra-médullaire. Les antalgiques opioïdes sont classées  selon leur action au niveau des récepteurs opioïdes, ainsi nous distinguons plusieurs classes :

- Action agoniste : les agonistes purs comme la morphine vont directement sur les récepteurs opioïdes et reproduisent tous les effets de la morphine, en augmentant les doses on peut atteindre un effet maximal.

- Action agoniste/antagoniste ou agoniste partiel : ils ont une efficacité limitée car ils ont un effet plafond même si l'on augmente les doses . Ils ne reproduisent pas tous les effets de  la morphine et s'ils prennent la place d'un agoniste pur ils en réduisent l'effet.

- Action antagoniste : (la Naloxone) Ils se fixent sur un des récepteurs opioïdes mais ne l'activent pas et empêchent les agonistes d'agir. C'est donc l'antidote de la morphine en cas d'intoxication.

Mais la morphine a en plus de ses effets antalgiques des propriétés pharmacologiques à l'origine le plus souvent d'effets indésirables à type de constipation, nausées, vomissements et par son action sur les récepteurs mu, elle peut entraîner une dépression respiratoire ( bronchoconstriction) et un effet sédatif. Une autre action sur des récepteurs opioïdes sigma explique l'effet psychologique c'est à dire une perturbation de l'activité mentale , ce qui explique le détournement de certains médicaments par les toxicomanes. La morphine est peu modifiée dans l'organisme, elle est surtout excrétée dans l'urine en nature et sous forme conjuguée.

b) Principes d'utilisation

NOMS

PRÉSENTATION

PUISSANCE (par rapport à la morphine)

POSOLOGIE

DURÉE D'ACTION

AGONISTE

MORPHINE

Buvable: ampoule 5-10-20 mg dans 10 ml

Per os: SKENAN et MOSCONTIN gel 10-30-60 mg

IV ou SC: ampoules  10-20-50 mg dans1-2-5 ml

Intra-rachidien: ampoule de 1 mg dans 1 ml

1

IV par PCA : 20 à 60 mg/24 h

4 à 6 H

FENTANYL

IV: ampoule de 500-100 mcg dans 10-2 ml

50 à100

Anesthésie: 3 à 5 mcg/kg

Sédation: 50 à 200 mg/h

20 à 30 min

PHENOPERIDINE    (R 1406) 

IV: ampoule de 10-2 mg dans 10-2 ml

10 à 15

Anesthésie: 40 mcg/kg

Sédation: 0.5 à 2 mg/h

40 min

ALFENTANIL (Rapifen)            

IV: ampoule de 5-1 mg dans 10-2 ml

30

40 à 100 mcg/h

10 min

SUFENTANIL  (Sufenta)

IV: ampoule de250 mcg dans 5 ml

700 à 1000

Anesthésie : 1 mcg/kg

Sédation: 0.5 à 1 mcg/kg/h

60 min

AGONISTE/ANTAGONISTE

NALBUPHINE (Nubain)

IV/IM: ampoule de  2 ml/20mg

2

Adulte:0.2 à 0.3 mg/kg (max 4 fois/24 h)

3 h

BUPREMORPHINE (Temgésic)

Sublinguale: Glossettes 0.2mg IV/IM: ampoule de  1 ml/0.3 mg

30

1 ampoule/12 h

6 h

ANTAGONISTE

NALOXONE

(Narcan)

IV: ampoule de 1 ml/ 0.4mg

 

Pour réverser une morphinisation faire 1 mcg/kg puis entretenir par perfusion

45 mn

c) Action et indications

FAMILLE

NOM

ACTION

CONTRE INDICATION

EFFETS SECONDAIRES

AGONISTES

MORPHINE

Moscontin, Skénan, Chlorhydrate de morphine

antalgique puissant

allergie à la morphine

insuffisance respiratoire

syndrome abdominal aigu d'étiologie inconnue

insuffisance hépato-cellulaire grave

trauma crânien, hypartension intra-crânienne

état convulsif

alcoolisme aigü, délirium tremens

analgésie, psychodyslepsie, sédation

actions respiratoires dose-dépendantes: bradypnée, apnée centrale, broncho-constriction, dépression de la toux

actions cardio-vasculaires: bradycardie, hypotension artérielle si hypovolémie

actions digestives: vomissements, stase gastrique, diminution du péristaltisme, constipation

action neurologique: somnolence, excitation, dépendance physique et psychique, augmentation de la pression intra-crânienne

syndrome de sevrage: bâillement, mydriase, larmoiement, rhinorrhées, contraction musculaire, céphalées, asthénie, sudation, anxiété, irritabilité, insomnie, anorexie, nausées, vomissements, amaigrissement, douleurs diffuses, diarrhées, tachycardie, polypnée, hyperthermie, hypertension artérielle

PETHIDINE

Dolosal

antalgique

anti-spasmodique

nourrisson<30 mois

traitement aux IMAO

(en plus de celles de la morphine (voir ci -dessus)

hypotension orthostatique en plus des effets de la morphine (voir ci -dessus)

DEXTROMORAMIDE

Palfium

antalgique central puissant

enfant < 16 ans

(en plus de celles de la morphine (voir ci -dessus)

(ceux de la morphine (voir ci -dessus)

FENTANYL

Fentanyl

absence d'assistance respiratoire

allergie

dépression respiratoire ++

effets parasympatho - mimétiques : bradycardie, hypotension

rigidité musculaire surtout thoracique

nausées, vomissements

PHENOPERIDINE  

R 1406

absence d'assistance respiratoire

allergie

dépression respiratoire ++

effets parasympatho - mimétiques: bradycardie, hypotension

ALFENTANIL

Rapifen

absence d'assistance respiratoire

pneumopathie chronique obstructive

allergie

dépression respiratoire

effets cholinergiques

SUFENTANIL 

Sufenta

absence d'assistance respiratoire

allergie

dépression respiratoire ++

effets parasympatho - mimétiques : bradycardie, hypotension

rigidité musculaire surtout thoracique

nausées, vomissements

AGONISTE/ANTAGONISTES

NALBUPHINE

Nubain

antalgique

allergie à la nalbuphine

syndrome chirurgical abdominal avant le diagnostic

nourrisson< 18 mois

actions neurologiques: somnolence, céphalées, troubles de l'humeur, sédation

actions digestives:             nausées , vomissements

actions cholinergiques: hypersudation, sécheresse buccale, bouffées vasomotrices

actions respiratoires:  risque de dépression respiratoire chez le nouveau- né  au cours d'une utilisation prolongée

BUPREMORPHINE

Temgésic

allergie au composant

insuffisance respiratoire sévère

insuffisance hépatique sévère

alcoolisme chronique voire délirium tremens

actions digestives: constipation, nausées, vomissements

actions neuro-psy: insomnie, asthénie, somnolence, lipothymie, sensations vertigineuses, rarement hallucinations et dépendance psychique et physique

actions respiratoires:  dépression respiratoire

ANTAGONISTES

NALOXONE

Narcan

antidote du surdosage à la morphine

morphino - mimétique

état de dépendance aux morphino - mimétiques

insuffisance cardiaque ou coronarienne grave et hypertension artérielle

allergie

syndrôme de sevrage: (chez personnes dépendantes aux opiacés) frissons, agitations, anxiété, hyperventilation, nausées, vomissements, tachycardie

NALORPHINE

Nalorphine

toxicomanie aux morphiniques

insuffisance hépatique sévère

insuffisance respiratoire

grossesse

actions digestives:             nausées, vomissements

actions neuro- psy:   bradycardie, myosis, lourdeur des membres

surdosage: troubles psychiques, sédation, dysphorie, irritabilité, anxiété, désorientation, hallucinations visuelles

syndrome de sevrage: hypersécrétion, anorexie, diarrhée, fièvre, tachypnée, prurit, sensation de choc électrique dans la tête, absence de quête compulsive

III. Traitements co-analgésiques

1°/ Les antidépresseurs

a) actions

Les antidépresseurs corrigent l'insuffisance en amines biogènes au niveau des synapses encéphaliques.

Il en existe deux grands groupes, les IMAO (inhibiteurs de la monoamine oxydase) et les tricycliques, plus de nouvelles familles non IMAO, non Tricycliques.

Ils ont une indications première de soigner le syndrome dépressif en diminuant les symptômes ( tristesse, perte d'intérêt, insomnie, anorexie, ralentissement moteur et psychique, apathie...)

b) indications

Dans le cadre de l'analgésie , ils sont utilisés dans les algies rebelles pour traiter les dépressions réactionnelles au phénomène douloureux et peut-être par une action antalgique non démontrée.

2°/ Les anti-spasmodiques

a) actions

Les anti-spasmodique agissent au niveau des muscles lisses du tube digestif , des voies urinaires et du muscle utérin. Il existe deux famille d'anti-spasmodiques:

les musculotropes et les anticholinergiques

Les anticholinergiques font la différence puisqu'ils vont entraîner le ralentissement de la vidange gastrique, diminuer les sécrétions gastriques, salivaires, lacrymale, sudorale en plus de leur action de départ. Ils vont aussi permettre une résorption digestive rapide mais entraîne une inactivation hépatique partielle.

Ils passent tous deux la barrière placentaire et vont dans le lait maternel.

b) indications

Ils sont utilisés essentiellement dans les syndrome douloureux des voies digestives, urinaires, biliaires et de la sphère génitale mais aussi dans la préméditation anesthésique pour la protection des manifestations cardiaques vagales

3°/ Les myorelaxants

a) actions

Ils ont une action de relaxation musculaire par l'inhibition des réflexes médullaires polysynaptiques ou au niveau réticulaire. Certains ont une action anti-spastique surajoutée

b) indications

Se  retrouvent dans le traitement des affections rhumatologiques à types de contractures musculaires douloureuses au cours d'affections vertébrales(torticolis, dorsalgies, lombalgies), dans des états spastiques ou dans les dysménorrhées et ils sont de plus en plus utilisés dans les traitements des états spastiques de la sclérose en plaques.

 

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