Добавил:
Sekretar
kiopkiopkiop18@yandex.ru
t.me/Prokururor I Вовсе не секретарь, но почту проверяю
Опубликованный материал нарушает ваши авторские права? Сообщите нам.
Вуз:
Предмет:
Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5282_Библиотеки_им_академика_М_И_Перельмана
.pdf
165
Anti-infective
Agents
Ganciclovir (GCV)
Structure:
NHN
N
N
O
NH2
O
OH
OH
Chemical name: 2-Amino-9-{[(1,3-dihydroxypropan-2-yl)-oxy]methyl}-6,9-dihydro-3H-
purin-6-one.
Uses: It is used in the treatment of sight-threatening CMV retinitis in severely immuno-
compromised patients.
CMV pneumonitis in bone marrow transplant recipients
Prevention of CMV disease in bone marrow and solid organ transplant recipients
Confirmed CMV retinitis in people with AIDS (intravitreal implant)
Formulations: Tablet and Injectable.
Brand name: Ganguard.
Oseltamivir
Structure:
O
O
N
H
O
NH
2
O
Chemical name: Ethyl-(3R,4R,5S)-5-amino-4-acetamido-3-(pentan-3-yloxy)-cyclohex-1-
ene-1-carboxylate.
Uses: It is used in the treatment and prevention of influenza caused by influenza A and B
viruses. It is the drug of choice in Swine flu (H1N1 infection).
NH
2
166
A Textbook of Pharmaceutical
Chemistry
Formulations: Capsule and Injectable.
Brand names: Tamiflu and Fluvir.
Foscarnet
Structure:
P
O
H
HO
O
O
OH
Chemical name: Phosphonoformic acid.
Uses: It is used in the treatment of herpes viruses including drug-resistant cytomegalovirus
(CMV) and herpes simplex virus types 1 and 2 (HSV-1 and HSV-2). It is particularly used to treat
CMV retinitis.
Formulations: Capsule and Injectable.
Brand name: Foscavir.
Ribavirin
Structure:
N
N
N
O
NH
2
O
OH
OH
OH
Chemical name: 1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-1H-
1,2,4-triazole-3-carboxamide.
Uses: It is useful in the treatment of hepatitis C and viral hemorrhagic fever.
Formulations: Capsule, Tablet and Syrup.
Brand names: Ribavin and Virazide.
167
Anti-infective
Agents
Zidovudine (AZT)
Structure:
N
HN
O
O
O
OH
N
3
Chemical name: 1-[(2R,4S,5S)-4-azido-5-(hydroxymethyl)-oxolan-2-yl]-5-
methylpyrimidine-2,4-dione.
Uses: AZT is usually dosed twice a day in combination with other antiretroviral therapies.
This approach is referred to as Highly Active Antiretroviral Therapy (HAART).
Formulations: Capsule and Tablet.
Brand names: Zidomax and Zydowin.
Lamivudine
Structure:
N
N
O
H
2
N
O
S
OH
Chemical name: 4-Amino-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-1,2-
dihydropyrimidin-2-one.
Uses: It is used in the treatment of chronic hepatitis B at a lower dose than for treatment of
HIV/AIDS.
Formulations: Capsule and Tablet.
Brand names: Zidomax and Zydowin.
Approved New Drugs
Daclatasvir (Daklinza)
Mechanism of action: It is the inhibitor of the hepatitis C virus (HCV) nonstructural
protein 5A (NS5A) replication complex. It is used to treat chronic hepatitis C virus (HCV)
genotype 3 infections.
168
A Textbook of Pharmaceutical
Chemistry
Xofluza (Baloxavirmarboxil)
Mechanism of action: It inhibits the cap-dependent endonuclease activity of the influenza
polymerase. It inhibits the process known as cap snatching.
It is used for the treatment of acute uncomplicated influenza.
Heplisav-B [Hepatitis B Vaccine (Recombinant)]
It is used for the prevention of hepatitis B virus infection.
Juluca (Dolutegravir and Rilpivirine)
Mechanism of action: It inhibits HIV integrase by binding to the active site and blocking
the strand transfer step of retroviral DNA integration in the host cell.
It is used in the treatment of HIV-1 infection.
KedRab [Rabies Immune Globulin (Human)]
It is used for the post-exposure prophylaxis of rabies infection.
Glecaprevir and Pibrentasvir (Mavyret)
Mechanism of action: It is the first pan-genotypic NS3/4A serine protease inhibitor
It is used for the treatment of chronic HCV genotype 1, 2, 3, 4, 5, or 6.
Letermovir (Prevymis)
Mechanism of action: It inhibits terminase complex.
It is used in the prevention of cytomegalovirus infections. Letermovir has received both
priority and orphan drug status from the FDA in 2017.
Shingrix (Zoster Vaccine Recombinant)
It is used for the prevention of herpes zoster (shingles).
Revcovi (Elapegademase-lvlr)
It is used for the treatment of adenosine de-aminase severe combined immune deficiency.
Rituxan (Rituximab)
Mechanism of action: It induces complement-mediated cytotoxicity and antibody-
dependent cell-mediated cytotoxicity
It is used in the treatment of infections caused by Pemphigus vulgaris.
Dengvaxia (Dengue Tetravalent Vaccine, Live)
It is useful for the prevention of dengue fever.
169
Anti-infective
Agents
13.5 ANTIMALARIAL AGENTS
mal-bad; aria-air
In humans, malaria is caused by the infection with protozoan parasites of the genus,
Plasmodium. These parasites spend a sexual phase in female Anopheles mosquitoes and an
asexual phase in a human. Out of several hundred known Plasmodium species, four species infect
humans. These are:
1. Plasmodium falciparum: It causes a malignant tertian form of malaria which may cause
death by invading the central nervous system. About half of the cases of malaria are
caused by this species. In this type, the attacks are more severe and recovery does not
occur.
2. Plasmodium vivax: It causes a benign tertian form of malaria in which fever revisits
patient every 48 hours. About 40% of the cases of malaria are caused by this species.
3. Plasmodium malariae: It is responsible for the occurrence of a quartan form of malaria
in which fever repeats after every 72 hours. It is a milder form of infection.
4. Plasmodium ovale: It is responsible for the mild tertian form of malaria which is most
commonly seen in West Africa.
Out of these species, P. falciparum and P. vivax pose the greatest threat.
Symptoms
Malaria is an acute febrile illness. In a non-immune individual, symptoms appear seven days
or more (usually 10–15 days) after the infective mosquito bite. The preliminary symptoms – fever,
headache, chills, and vomiting may be mild and difficult to recognize as malaria. If not treated
within 24 hours, P. falciparum malaria can progress to severe illness, often leading to death.
Antimalarial drugs are classified as follows:
(a) 4-Amino quinolines
Chloroquin
Amodiaquine
Piperaquine
(b) 8-Amino quinolines
Primaquine
(c) Biguanides
Proguanil
Cycloguanil (Proguanil)
170
A Textbook of Pharmaceutical
Chemistry
(d) Diaminopyrimidine
Pyrimethamine
(e) Cinchona alkaloids
Quinine
(f) Sesquiterpene lactones
Artesunate
Artemether
Arteether
(g) Aminoalkaloids
Halofantrine
Lumefantrine
(h) Quinoline methanol
Mefloquine
(i) Naphthoquinone
Atovaquone
Quinine
Structure:
OH
N
H
O
N
Chemical name: (R)-(6-Methoxyquinolin-4-yl)[1S,2S,4S,5R)-5-vinylquinuclidin-2-yl]-
methanol
Uses: As an antimalarial agent. It is the drug of choice for cerebral malaria.
Formulations: Tablet and Injectable.
Brand names: Quinine and Rezoquin.
171
Anti-infective
Agents
Chloroquine
Structure:
N
Cl
HN
N
Chemical name: (RS)-N’-(7-Chloroquinolin-4-yl)-N,N-diethylpentane-1,4-diamine.
Uses: To treat malaria. It is the drug of choice for malaria caused by P. falciparum. It is
useful in rheumatoid arthritis. In the treatment of an amoebic liver abscess.
Formulations: Tablet, Suspension and Injectable.
Brand names: Lariago, Cloquin and Nivaquin-P.
Primaquine
Structure:
N
O
HN
NH
2
Chemical name: (RS)-N-(6-Methoxyquinolin-8-yl)-pentane-1,4-diamine.
Uses: It is used in the treatment of Pneumocystis pneumonia (PCP), a fungal infection
commonly occurring in people with AIDS. To prevent relapse of malaria due to P. vivax and P.
ovale.
Formulations: Tablet and Injectable.
Brand names: Malirid and Evaquin.
172
A Textbook of Pharmaceutical
Chemistry
Mefloquine
Structure:
N
F F
F
F
F
F
HO
HN
H
Chemical name: [(R,S)-2,8-bis-(trifluoromethyl)quinoline-4-yl]-(2-piperidyl)methanol.
Uses: It is useful for the prevention of malaria in all areas except for those where parasites
may have resistance to multiple drugs. It is used as a treatment for chloroquine sensitive or
resistant P. falciparum malaria.
Formulations: Tablet and Injectable.
Brand names: Mefliam, Lariam, and Mephaquin.
Proguanil
Structure:
Cl
N
H
HN
HN
NH
NH
Chemical name: 1-[Amino-(4-chloroanilino)-methylidene]-2-propan-2-ylguanidine.
Uses: It is used for the prevention and treatment of malaria in both adults and children.
Formulations: Tablet and Injectable.
Brand name: Progumal.
Cycloguanil is an active metabolite of proguanil which is a dihydrofolate reductase inhibitor
and responsible for antimalarial activity.
173
Anti-infective
Agents
Pyrimethamine
Structure:
N
N
Cl
H
2
N NH
2
Chemical name: 5-(4-Chlorophenyl)-6-ethyl-2,4-pyrimidinediamine.
Uses: It is used in the treatment of malaria. Pyrimethamine is also used in combination with
sulfadiazine to treat active toxoplasmosis. (Toxoplasmosis is a parasitic disease caused by
Toxoplasma gondii).
Formulations: Tablet and Injectable.
Combination: Sulfamethopyrazine + Pyrimethamine (500:25 mg).
Brand names: Laridox and Fancidar.
Approved New Drugs
Arterolane Maleate and Piperaquine Phosphate Combination
Mechanism of action: It causes inhibition of heme detoxification. The artemisinin
component produces a rapid reduction of parasitemia by 100- to 1000-fold per asexual cycle of
the parasite, and complete clearance is dependent on the long-acting partner drug.
Ferroquine
Mechanism of action: It inhibits the formation of hemozoin and generates reactive oxygen
species.
13.6 ANTI-AMOEBIC AGENTS
Amoebiasis (also called amebic dysentery) is an infection of the intestinal tract caused by
Entamoeba histolytica. The disease can be acute or chronic, with the patients showing varying
degrees of illness, from no symptoms to mild diarrhea to fulminating dysentery (Dysentery in
which the symptoms are intensely acute, leading to prostration, collapse, and often death).
Protozoal infections are common among people in under-developed tropical and subtropical
countries, where sanitary conditions, hygienic practices, and control of vectors of transmission are
inadequate.
174
A Textbook of Pharmaceutical
Chemistry
Entamoeba histolytica exists in two forms:
1. Cysts form (That can survive outside the body).
2. Trophozoites form (That are labile and don’t persist outside the body).
Drugs used to treat amebiasis are called antiamebic drugs. They are classified as:
(a) Nitroimidazole Derivatives
Metronidazole
Tinidazole
Secnidazole
Benznidazole
Ornidazole
Nimorazole
(b) Dichloroacetamide Derivatives
Diloxanidefuroate
Clefamide
Teclozan
Etofamide
(c) 4- aminoquinoline Derivatives
Chloroquine
(d) Alkaloids of Ipecacuanha
Emetine (very toxic)
Dehydroemetine (less toxic)
(e) Antibiotics
Tetracycline
Paromomycin
Erythromycin
Соседние файлы в папке Библиотека им академика М.И. Перельмана