Antihistamin

 Ismar
• Jelaskan mekanisme kerja antihistamin gol H1?
 Vini
• Bagaimana memperlakukan difenhidramin? Kalau
ada penyalahgunaan, bagaimana cara
mengatasinya?
 Sri Kartila
• Apakah antagonis H1 & H2 mempunyai efek yg sama?
 Ria Lestari
• Reaksi pembuatan CTM?
 Achsa
• Menghambat secara langsung dan bersaing
kerja histamin pada reseptor yang mengandung
reseptor H1.
 Jules
• Sedatif & antikolinergik. Setelah mengonsumsi
tidak mengendarai. Penanggulangannya:
Menjelaskan lebih dalam karena efek
sampingnya kantuk.
 Icha
• ESOnya berbeda.
• Contoh difenhidramin antikolerik. H2 simetidin,
efek sampingnya diare.
• Berbeda karena sesuai dengan cara kerja
masing2.
 an organic nitrogen compound
 involved in local immune response as
well as regulating physiological function
 acting as a neurotransmitter
 triggers the inflammatory response
 As part of an immune response to foreign
pathogens
 produced by basophils and by mast cells
found in nearby connective tissues
 N

NH2
HN
Disintesis melalui dekarboksilasi asam
amino histidin.
Reaksinya dikatalis dengan enzim L-
histidine decarboxylase
Receptor Function Antagonist

H1 ileum contraction, modulate circadian Dipenhydramine,

cycle, itching, systemic vasodilatation, Loratadine, Cetirizine,
bronchoconstriction (allergy-induced Fexofenadine,
asthma) Clemastine
H2 speed up sinus rhythm, Stimulation of Ranitidine, Cimetidine,
gastric acid secretion, smooth muscle Famotidine, Nizatidine
relaxation, Inhibit antibody synthesis,
T-cell proliferation and cytokine
production
H3 Decrease Acetylcholine, Serotonin ABT-239, Ciproxifan,
and Norepinephrine neurotransmitter Clobenpropit,
release in CNS, Presynaptic Thioperamide
autoreceptors
H4 mediate mast cell chemotaxis. Thioperamide,
JNJ7777120
Type Location Function
H1 smooth muscle, Causes bronchoconstriction, bronchial smooth
endothelium, and CNS muscle contraction, vasodilation separation of
endothelial cells (responsible for hives), and pain
and itching due to insect stings; the primary
receptors involved in allergic rhinitis symptoms
and motion sickness; sleep and appetite
suppression.
H2 parietal cells and Primarily involved in vasodilation. Also stimulate
vascular smooth muscle gastric acid secretion
cells
H3 CNS and peripheral Decreased neurotransmitter release: histamine,
nervous system acetylcholine, norepinephrine, serotonin

H4 Basophils and in the bone Plays a role in chemotaxis.

marrow. It is also found
on thymus, small
intestine, spleen, and
colon.
 Histamin dilepaskan sebagai
neurotransmitter
 Neuron yang melepaskan histamin
ditemukan di hipotalamus posterior
 Histaminergik diketahui memiliki
peranan dalam proses tidur.
 Sebaliknya antagonis H3 memiliki efek
yang ‘membangunkan’.
 Merupakan antagonis dari histamin pada
reseptor H1
 Berfungsi untuk mengurangi atau
mengeliminasi efek dari histamin
 Antihistamin mengacu pada H1
antagonis.
 Histamin, yang bekerja pada reseptor H1
menyebabkan gatal, vasodilatasi,
hipotensi, pusing, dan sesak nafas
 While H1-antihistamines help against
these effects, they work only if taken
before contact with the allergen
 Adverse drug reactions are most
commonly associated with the first-
generation H1-antihistamines. This is due
to their relative lack of selectivity for the
H1-receptor and their ability to cross the
blood-brain barrier (BBB)
 The most common adverse effect is
sedation; this "side-effect" is utilized in
many OTC sleeping-aid preparations
 The newer, second-generation H1-
antihistamines are far more selective for
peripheral histamine H1-receptors and
have a far better tolerability profile
compared to the first-generation age
 A second method starts from Pyridine
 Undergoes alkylation by 4-
chlorobenzylchloride
 Giving 2-(4-chlorobenzyl)pyridine.
 Alkylating this with 2-
dimethylaminoethylchloride in the
presence of sodium amide gives
chlorphenamine.
Diuretik
 Putri
• Bagaimana cara kerja diuretik dalam terapi
edema
 Julestari Putri
• Syarat obat ‘Umumnya resisten terhadap
perubahan-perubahan metabolik’ – slide 11,
makalah hal 8
• Bagaimana sintesis Manitol?
 Anggi
• Peraturan khusus dalam penggunaan diuretik?
 Nurjanah
• Edema – peningkatan cairan
• Menghambat kotransport Na K ATP
 Lestari
• Furosemid – terdapat tindakan khusus.
Mengonsumsi makanan rendah natrium, diet
rendah garam. Beri selang 1 jam kolestikol
setelah minum furosemid.
A diuretic is any substance that
promotes the production of urine.
 All diuretics increase the excretion of
water from bodies, although each class
does so in a distinct way.
 Diuretics are used to treat heart failure,
liver cirrhosis, hypertension, water
poisoning, and certain kidney diseases.
 Edema is swelling caused by excess fluid
trapped in your body's tissues.
 Although edema can affect any part of
your body, it's most commonly noticed in
the hands, arms, feet, ankles and legs.
 Edema can be the result of medication,
pregnancy or an underlying disease —
often heart failure, kidney disease or
cirrhosis of the liver.
 Mild edema usually goes away on its own.
 More severe edema may be treated with
drugs that help your body expel excess
fluid in the form of urine (diuretics). One of
the most common diuretics is furosemide
(Lasix).
 Long-term management typically focuses
on treating the underlying cause of the
swelling. If edema occurs as a result of
medication use, your doctor may adjust your
prescription or check for an alternative
medication that doesn't cause edema.
 An osmotic diuretic is a type of diuretic
that inhibits reabsorption of water and
sodium (Na).
 They are pharmacologically inert
substances that are given intravenously.
 They increase the osmolarity of blood
and renal filtrate.
 Mannitol is commonly produced via the
hydrogenation of fructose, which is formed from
either starch or sucrose.
 Sucrose is simply hydrolyzed into an invert sugar
syrup, which contains about 50% fructose.
 In both cases, the syrups are chromatographically
purified to contain 90–95% fructose.
 The fructose is then hydrogenated over a nickel
catalyst into mixture of isomers sorbitol and
mannitol.
 Yield is typically 50%:50%, although slightly alkaline
reaction conditions can slightly increase mannitol
yields.