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Methatmpyrone sinonim :
1-phenyl-3-pyrazolin-4-yl)-N-methylaminomethanesulphonate
monohydrate.
(martindale)
Hayooo apalagi
(Japanese Pharmacopeia)
C13H16N3NaO4S,H2O 351.4
(british pharmacopeia)
Pemerian :
A white or almost white, crystalline powder, very soluble in water, soluble in alcohol.
(Japanese Pharmacopeia) A white or almost white crystalline powder. Very soluble in water; soluble
(martindale)
Bubuk kristal putih atau hampir putih, sangat larut dalam air, larut dalam alkohol.
(Japanese Pharmacopeia) Bubuk kristal putih atau hampir putih. Sangat larut dalam air; larut
dalam alkohol. Lindungi dari cahaya.
(british pharmacopeia)
Stabilitas :
Dosis : Oral or intranasal administration. For oral, the adult should take 0.5g of the medicine and three
times a day, the amount of the child is 8-10mg/ kg, the number of the times is according to the
necessary. For intranasal, the child under 5 years old can take 1-2drops for each nostril, can take the
medicine another time if necessary,for the patient above 5 years old increase the dosage appropriately.
http://www.chemicalbook.com/ChemicalProductProperty_EN_CB7741339.htm
oral dose of 0.5 to 1 gram.'
Administrasi lisan atau intranasal. Untuk oral, orang dewasa harus minum 0,5g obat dan tiga kali sehari,
jumlah anak 8-10mg / kg, berapa kali sesuai kebutuhan. Untuk intranasal, anak di bawah 5 tahun dapat
minum 1-2drop untuk setiap lubang hidung, dapat minum obat lain jika diperlukan, karena pasien di
atas 5 tahun meningkatkan dosisnya dengan tepat.
Farmakologi :
Irrespective of the inhibition of PGE2 synthesis, other mechanisms participate in the production of
theanalgesic effect of metamizole.It is a well-known fact that activation of CB1 receptors reduces
GABAergic transmission in periaqueductal grey matter (PAG), which disinhibits activating neurons
(mainly glutaminergic ones) and initiates antinociception, as a consequence of the activation of the
descending pathway (Rutkowska and
Metamizole (dipyrone) is a popular analgetic, non-opioid drug, commonly used in human and veterinary
medicine. In some cases, this agent is still incorrectly classified as a non-steroidal anti-inflammatory drug
(NSAID). Metamizole is a pro-drug, which spontaneously breaks down after oral administration to
structurally related pyrazolone compounds. Apart from its analgesic effect, the medication is an
antipyretic and spasmolytic agent. The mechanism responsible for the analgesic effect is a complex one,
and most probably rests on the inhibition of a central cyclooxygenase-3 and activation of the opioidergic
system and cannabinoid system. Metamizole can block both PG-dependent and PG-independent
pathways of fever induced by LPS, which suggests that this drug has a profile of antipyretic action
distinctly different from that of NSAIDs. The mechanism responsible for the spasmolytic effect of
metamizole is associated with the inhibited release of intracellular Ca2+ as a result of the reduced
synthesis of inositol phosphate. Metamizole is predominantly applied in the therapy of pain of different
etiology, of spastic conditions, especially affecting the digestive tract, and of fever refractory to other
treatments. Co-administration of morphine and metamizole produces superadditive, antinociceptive
effects. Metamizole is a relatively safe pharmaceutical preparation although it is not completely free
from undesirable effects. Among these side-effects, the most serious one that raises most controversy is
the myelotoxic effect. It seems that in the past the risk of metamizole-induced agranulocytosis was
exaggerated. Despite the evidence showing no risk of teratogenic and embryotoxic effects, the drug
must not be administered to pregnant women, although it is allowed to be given to pregnant and
lactating animals. This paper seeks to describe the characteristics of metamizole in the light of current
knowledge.
https://www.ncbi.nlm.nih.gov/pubmed/24724493
Pharmacological characteristics of
metamizole.
Jasiecka A, Malanka T, Jaroszewski JJ.