Kimia Farmasi

Antihistamin
 Ismar
• Jelaskan mekanisme kerja antihistamin gol H 1?
 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.
 Histamine
 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
 Histamine
N

NH2
HN
 Synthesis

Disintesis melalui dekarboksilasi

asam amino histidin.
Reaksinya dikatalis dengan enzim L-
histidine decarboxylase
 Antagonis
Recept Function Antagonist
or
H1 ileum contraction, modulate Dipenhydramine,
circadian cycle, itching, systemic Loratadine, Cetirizine,
vasodilatation, bronchoconstriction Fexofenadine,
(allergy-induced asthma) Clemastine
H2 speed up sinus rhythm, Ranitidine,
Stimulation of gastric acid Cimetidine,
secretion, smooth muscle Famotidine,
relaxation, Inhibit antibody Nizatidine
synthesis, T-cell proliferation and
cytokine production
H3 Decrease Acetylcholine, Serotonin ABT-239, Ciproxifan,
and Norepinephrine Clobenpropit,
neurotransmitter release in CNS, Thioperamide
Presynaptic autoreceptors
H4 mediate mast cell chemotaxis. Thioperamide,
JNJ7777120
 Receptor
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
vascular smooth stimulate gastric acid secretion
muscle cells
H3 CNS and peripheral Decreased neurotransmitter release:
nervous system histamine, acetylcholine, norepinephrine,
serotonin
H4 Basophils and in the Plays a role in chemotaxis.
bone marrow. It is also
found on thymus, small
intestine, spleen, and
colon.
 Sleep regulation
 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’.
 H1 Antagonis
 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
 H1 Antagonis
 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)
 H1 Antagonis
 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.
Kimia Farmasi
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.
 Diuretic
 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
 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
 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.
 Osmotic Diuretic
 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
 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.
Mannitol