Unit 2 MEDICINAL CHEMISTRY – III Typing Notes B.Pharmacy

 

UNIT II

 

Macrolide: Erythromycin, Clarithromycin, Azithromycin.

(i) Erythromycin:-

1)    is an antibiotic used for the treatment bacterial infections.

2)    it belongs to a group macrolide antibiotics.

3)    Slows the growth or kills bacteria by reducing the production of important proteins needed by the bacteria to live.

Mechanism of action:-

       Inhibit  Protein synthesis by binding to the 23S ribosomal RNA molecule .

Uses:-

       Used in respiratory tract, ear, nose, throat, lungs, and skin infections.

Side effects :-

1)    nausea

2)    vomiting

3)    loss of appetite

4)    diarrhea

5)    abdominal pain.

 

(Write Same for  Clarithromycin, Azithromycin and include  Pharmacokinetics ,Pharmacodynamics  and Excretion through Urine etc.)

 

 

 

Miscellaneous : Chloramphenicol*, Clindamycin.

(i) Chloramphenicol:-

1)    It is an antibiotic.

2)    is a semi-synthetic  broad-spectrum antibiotic.

3)    It is mainly used to treat eye infections (such as conjunctivitis) and  ear infections.

4)    It comes as eye drops and eye ointment.

 

    Mechanism of action:-

          Inhibit  the protein synthesis by binding with ribosomes.

    Absorption:-

       Rapidly and completely absorbed from gastrointestinal  tract  following oral administration (bioavailability 80%)

    Side effects :-

1)    nausea

2)    vomiting

3)    loss of appetite

4)    diarrhea

5)    abdominal pain.

(ii) Clindamycin:-

1)    it is used to treat bacterial infections.

2)    It is used to treat infections of the lungs, skin, blood, female reproductive organs, and internal organs.

 

Mechanism of action:-

     Binds to the 50s ribosomal  subunit of bacteria.

 Side effects :-

1)    nausea

2)    vomiting

3)    loss of appetite

4)    diarrhea

5)    abdominal pain.

Q. Basic concepts and application of pro-drugs design

Ans.

1)    Prodrugs are derivatives of active drug.

2)    After metabolized converts into active drug.

Application:-

1)    Improvement  of taste

2)    Improvement  of odour

3)    Reduction of  irritation

4)    Reduction of pain on injection

5)    Enhancement of drug solubility and dissolution rate

6)    Enhancement of chemical stability of drug.

7)    Enhancement of provability

8)    Prevention of pre-systemic metabolism

9)    Prolongation of duration of action

               

 

Q. Etiology/Cause of malaria:-

Ans.

1)    Plasmodium falciparum – mainly found in Africa, it's the most common type of malaria parasite and is responsible for most malaria deaths worldwide

2)    Plasmodium vivax – mainly found in Asia and South America, this parasite causes milder symptoms than Plasmodium falciparum, but it can stay in the liver for up to 3 years, which can result in relapses

3)    Plasmodium ovale – fairly uncommon and usually found in West Africa, it can remain in your liver for several years without producing symptoms

4)    Plasmodium malariae – this is quite rare and usually only found in Africa

5)    Plasmodium knowlesi – this is very rare and found in parts of southeast Asia

 

 

 

 

Quinolines: SAR, Quinine sulphate, Chloroquine*, Amodiaquine, Primaquine phosphate, Pamaquine*, Quinacrine hydrochloride, Mefloquine.

 

(i) Quinine sulphate:-

1)    It is an antimalarial drug.

2)    Used to treat malaria caused by mosquito bites.

3)    used to kill the malaria parasites living inside red blood cells.

Mechanism of action:-

1)    Inhibit  nucleic acid synthesis.

2)    Inhibit  protein synthesis.

3)    Inhibit glycolysis in Plasmodium falciparum.

     Side effects :-

1)    nausea

2)    vomiting

3)    loss of appetite

4)    diarrhea

5)    abdominal pain

(ii) Chloroquine:-

1)    used to prevent and treat malaria.

2)    It is also used to treat liver infection caused by protozoa.

3)    also be used to treat coronavirus (COVID-19).

 

 

 

Mechanism of action:-

1)    inhibit the formation of hemozoin  from the heme which is released by the digestion of hemoglobin (Hb)

2)    The free heme then lyses membranes and  parasite death.

Side effects :-

1)    nausea

2)    vomiting

3)    loss of appetite

4)    diarrhea

5)    abdominal pain

(Write Same for  Amodiaquine, Primaquine phosphate, Pamaquine*, Quinacrine hydrochloride, Mefloquine. and include  Pharmacokinetics ,Pharmacodynamics  and Excretion through Urine etc.)

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Biguanides and dihydro triazines: Cycloguanil pamoate, Proguanil

 

(i)Cycloguanil pamoate:-

1)    It is an antimalarial drug.

2)    It is dihydrofolate reductase inhibitor.

3)     it is a metabolite of the antimalarial drug.

4)    Used to treat malaria caused by mosquito bites.

  Mechanism of action:-

1)   It is dihydrofolate reductase inhibitor.

2)    it is a metabolite of the antimalarial drug.

 

 Side effects :-

1)    nausea

2)    vomiting

3)    loss of appetite

4)    diarrhea

5)    abdominal pain.

(ii) Proguanil:-

1)    help to protect you from malaria when you travel.

2)    take the tablets one week before you travel.

3)    It is used in combination with another antimalarial drug to increase its effectiveness.

   Mechanism of action:-

         It works by stopping the malaria parasite from reproducing once it is in the red blood cells.

   Side effects :-

1)    nausea

2)    vomiting

3)    loss of appetite

4)    diarrhea

5)    abdominal pain

 

 

 

 

 

Miscellaneous: Pyrimethamine, Artesunete, Artemether, Atovoquone

 

(i)Pyrimethamine:-

1)    it is an antiparasitic drug .

2)    used in the prevention and treatment of toxoplasmosis and malaria.

3)    prevent infection in people with HIV infection.

    Mechanism of action:-

1)    inhibits the dihydrofolate reductase of plasmodia.

2)    it blocks the biosynthesis of purines and pyrimidines

3)    which are essential for DNA synthesis and cell multiplication.

Uses :-

1)    treat serious parasite infection (toxoplasmosis) of the body, brain, or eye

2)    prevent infection in people with HIV infection.

 Side effects :-

1)    nausea

2)    vomiting

3)    loss of appetite

4)    diarrhea

5)    abdominal pain.

6)    Headache.

 

 

 

 

 

(ii) Artesunete:-

1)    used to treat malaria.

2)    given by intravenous form for severe malaria.

 

Mechanism of action:-

1)    it is metabolized to active DHA.

2)    inhibit protein and nucleic acid synthesis.

Side effects :-

1)    nausea

2)    vomiting

3)    loss of appetite

4)    diarrhea.

5)    abdominal pain.

 

       (Write Same for Artemether)

(iii) Atovoquone:-

  Mechanism of action:-

      Inhibit the mitochondrial electron transport chain at the bc1 complex.

   (other points same as Artesunete)

 

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