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Bacteria can reproduce through binary fission and by exchanging their genetic material. Binary fission produces the daughter cells having the same characteristics as that of the parent cell. In the conjugation and transformation methods, two organisms are involved in the reproduction process.

Binary fission

Binary fission is the division of one parent organisms into two daughter bodies. This process takes place in two steps, i.e., replication of genetic material and division of parent body into two. The process takes place through following steps:

1. At the spot of origin, the DNA of bacteria started to replicate. In this process, the two parts moves towards the opposite ends of the cell, due to which, chromosome is also pulled. For adding the separation of the newly formed chromosomes, the cell gets longer.
2. On the completion of the division of the genetic material, the newly formed chromosome shifts to the opposite end of the cell and it begins the cytoplasm division process.
3. Cell membrane pinches inwards and the new dividing cell wall is formed in the middle of the cell.
4. The septum splits down in the middle to give rise to two individual cells.

Fig: Binary fission in bacteria

The above image is taken only for educational purpose from [1]

Conjugation

DNA is transferred from on bacteria to another through a structure called pilus. DNA in the form of plasmid is transferred from the donor (F⁺) cell to the recipient (F^–) cell. Donor cell has an additional F factor or fertility factor which can code for protein that can make the sex pilus. The following steps are involved in the process of conjugation:

1. Pilus is produced by The F+ or donor cell which starts to contact with the F- or Recipient cell.
2. There is direct contact between donor and recipient with the help of Pilus.
3. The T-strand is transferred to the recipient cell through the pilus.
4. In the final step, both donor and recipient cells replicate the single stranded DNA and forms double-stranded F-plamid.

Fig: Conjugation in bacteria

The above image is taken only for educational purpose from [1]

Transformation

In this process, the bacteria takes the DNA from the environment. When the DNA taken is in circular form, then it is called plasmid, which can be passed to the other generations. This technique in also used in laboratories for introducing new DNA fragments into the bacterial cells.

The process of bacterial transformation is very useful  in the molecular cloning. Multiple copies of recombinant DNA molecule can be formed by using transformation process.

Transduction

In this, the carrier for the DNA transfer is viruses. Viruses which infects the bacteria can carry small fragments of DNA from one bacterial cell to another. Viruses which can infect the bacterial cell are known as bacteriophages.

Fig: Transduction in bacteria

The above image is taken only for educational purpose from [1]

MCQs

1. Daughter cells produced from binary fission in bacteria have?

a. Same characteristics as that of the parent cell

b. Different characteristics as that of the parent cell

c. May have same of different characteristics as that of the parent cells

d. Bacteria cannot reproduce from binary fission

2. Genetic material is transferred from one bacteria to another bacteria in Bacterial conjugation with the help of?

a. Cilia

b. Flagella

c. Pilus

d. Mitochondria

3. Molecular cloning of recombinant DNA can be done by the help of?

a. Binary fission

b. Conjugation

c. Transformation

d. Transduction

4.Which Viruses are involved in the Bacterial Transduction process?

a. Animal viruses

b. Plant viruses

c. Bacteriophages

d. All of the above

5. Bacteria can reproduce through which method?

a. Binary fission

b. Conjugation

c. Transduction

d. All of the above

6. Transfer of genetic material can take place in bacteria through which method?

a. Transformation

b. Transduction

c. Conjugation

d. All of the above

7. Pilus is formed by which type of cell?

a. F⁺ 

b. F^–

c. Bacteriophages

d. Both a. and b.

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ANSWERS

1-a

2-c

3-c

4-c

5-d

6-d

7-a

RFERENCES

The post Bacterial Reproduction/Study material for Bacteria Chapter and MCQs for GPAT appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.

All the perfect fungi can reproduce sexually as well as asexually, but fungi imperfecti can only reproduce asexually. In sexual as well as in asexual reproduction, fungi forms spores, which are very light in weight and can be dispersed with the help of wind, water or animals.

Asexual reproduction

Majority of fungi reproduce asexually through formation of spores. While, some fungi can also reproduce asexually through budding and fragmentation. In fragmentation, mycelium is fragmented into pieces and each piece can grow into separate mycelium. Whereas, in budding, a bulge is formed on the side of the cell of fungi and nucleus divides mitotically. At the end, the bud detaches itself from the parent cell and can grow as an independent organism.

Fig: Budding in Yeast

The above image is taken only for educational purpose from [1]

Formation of spores during asexual reproduction includes mitosis divisions in which only one parent is required. Different types of spores can be produced by the fungi. Conidiospores are unicellular or multicellular and are released directly from the tip of the hypha. Sporangiospores are the spores produced in the sporangium. In the process of fragmentation, hypha forms unicellular cells which are then released in environment in form of spores. Individual grown from asexual spores are genetically identical to the parent organism.

Sexual reproduction

Sexual reproduction can only occur in the perfect fungi, while fungi imperfecti cannot exhibit sexual reproduction. In sexual reproduction, two mating types are required. Homothallic or self-fertile organisms have presence of both mating types on the same mycelium, heterothallic have presence of only one type of mating type in the mycelium and required two different types of mating times, which are compatible to reproduce sexually.

There are variations in the process of sexual reproduction in each class of fungi, but sexual reproduction in fungi include three common stages. They are:

1. Plasmogamy: In this, two haploid cells fuse together or there is union of the cytoplasm of two haploid cells. This results in the formation of a dikaryotic cell, in which, two haploid nuclei exist in the same cell.
2. Karyogamy: In this stage, two haploid nuclei fuse together to give rise to a diploid zygote.
3. Meiosis: Within the gametangia, gametes of different mating types are generated. These in the form of spores are disseminated into the environment.

Fig: Life cycle of a fungi

The above image is taken only for educational purpose from [1]

The life cycle of a typical perfect fingi can be understand by the example of life cycle of ascomycota class members. It involves:

i. It starts from haploid organism (N+N)

ii. Karyogamy which is the fusion of nuclei to produce diploid organism (2N)

iii. Meisos results in the formation of 8 ascospores in the ascus.

iv. Ascospores are released in environment which though mitosis, udergoes asexual reproduction and produces Male and Female strains separately.

v. Anthredium (male) and Archegonium (female) undergoes Cytoplasmic fusion (Karyogamy) to form the haploid organism known as Ascocarp.

Fig: Life cycle of ascomycota class members

The above image is taken only for educational purpose from [1]

MCQs

1. Number of parents required during formation of spores in fungi during asexual reproduction is?

a. 1

b. 2

c. 3

d. 4

2. Reproduction in fungi can be through?

a. Asexual reproduction only

b. Sexual reproduction only

c. Both sexual and asexual reproduction in all the classes of fungi

d. Asexual reproduction and sexual in most of the fungi

3. Sexual reproduction is not found in which class of fungi?

a. Ascomycota

b. Zygomycota

c. Basidiomycota

d. None of the above

4. Type of spore formed during asexual stage of Ascomycota is called?

a. Conidia

b. Ascospores

c. Zygospores

d.  Basidia

5. Deuteromycota class is also called as ‘Fungi Imperfecti’ as?

a. Hyphae is absent in them

b. They cannot move

c. Sexual reproduction is absent in them

d. They are non-pathogenic to human

6. Number of ascospores present in one ascus after completion of miosis is?

a. 1

b. 2

c. 4

d. 8

7. Correct sequence for the sexual cycle of fungi starting from the haploid organism can be?

I. Plasmogamy

II. Karyogamy

III. Miosis

IV. Mitosis

a. I – II – III

b. I – II – IV

c. IV – III – I

d. III – I – II

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ANSWERS

1-a

2-d

3-d

4-a

5-c

6-d

7-a

RFERENCES

The post Reproduction in Fungi/Microbiology Subjective notes for BPharm/MCQs for GPAT and NIPER appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.

Classification of bacteria on basis of their basic cell shapes

Cocci: Unicellular, spherical or elliptical shape.

• Monococcus: A single discrete round shape. Eg: Micrococcus flavus
• Diplococcus: Two spherical shaped bacteria attached with each other. Eg: Diplococcus pneumonia.
• Streptococcus: A chain of spherical bacteria attached with each other. Eg: Streptococcus pyogenes.
• Tetracoccus: Four round cells right angle to each other. Eg: Staphylococcus aureus.
• Sarcina: Eight or sixteen cells attached with each other in a cubic shape. Eg: Sarcina lutea

Bacilli: Rod shaped or cylindrical shaped bacteria may be present single or in pairs. Eg: Bacillus cereus.

Vibrio: Curved comma shaped bacteria. Eg: Vibrio cholera.

Spirilla: Bacteria present in spiral or spring like shape with multiple curvatures. Eg: Spirillum volutans.

(The image is taken from Black JG. Microbiology: principles and explorations  for education purpose only)

On the basis of growth characteristics

• On the basis of the requirement of oxygen for growth by microorganism [click here]
• On the basis of optimum temperature required by bacteria for proper growth [click here]
• On the basis of pH required for bacteria to grow properly [click here]
• On the basis of hydrostatic pressure required by bacteria for growth [click here]
• On the basis of osmotic pressure required by bacteria for its growth [click here]

On the basis of mode of nutrition

• Phototrophs: These bacteria gain energy from sunlight. They may get electrons from inorganic compounds (photolithotrophs), for eg.: Chromatium okenii, or may get electrons from organic compound (Photoorganotrophs).
• Chemotroph: These bacteria cannot carry photosynthesis and gains energy from chemical compounds. They can be further classified as chemolithotrophs (Nitrosomonas) and chemoorganotrophs (Pseudomonas pseudoflava)
• Autotrophs: These bacteria uses carbon dioxide as the source of carbon. They can be photoautotrophs and chemoautotrophs.
• Heterotrophs: Bacteria which cannot fix carbon dioxide and thus, uses other organic sources for food. Most of the human pathogens falls under this category.

On the basis of cell wall

• Gram-positive bacteria: Bacteria having thick layer of peptidoglycan in their cell wall.
• Gram-negative bacteria: Bacteria having thin layer of peptidoglycan in their cell wall.

• Acid fast bacteria: They have high lipid contains in their cell wall.

General characteristic of bacteria

Bacteria are unicellular prokaryotic organisms. Most of the species of bacteria are highly pathogenic in nature and causes human and animal diseases. They have a rigid cell wall, a cell membrane, nuclear region and 70S type of ribosomes. (click here for detailed information)

Structure of Bacterial Ribosome

Bacterial Cell Nuceloid Structure & Function

Bacterial Cell Capsule Structure & Function

Bacterial Cell Flagella Structure & Function

Bacterial Cell Pili Structure

MCQs

Q.1. Micrococcus flavus is an example of?

a) Monococcus bacteria

b) Diplococcus bacteria

c) Streptococcus bacteria

d) Tetracoccus bacteria

Q.2. Rod shaped bacteria are known as?

a) Vibrio

b) Spirilla

c) Bacilli

d) Cocci

Q.3. Bacteria which gain energy from sunlight  and get electrons from inorganic compounds are known as?

a) Photoorganotrophs

b) Photolithotrophs

c) Chemoorganotraphs

d) Chemolithotrophs

Q.4. Gram negative bacteria have?

a) Thick layer of peptidoglycan in cell wall

b) Thin layer of peptidoglycan in cell wall

c) High lipid contain in the cell wall

d) None of the above

Q.5. Bacteria have which type of ribosomes in their nuclear region?

a) 80S

b) 70S

c) 94S

d) 43S

Q.6. Which of  the following bacteria are the phototrophs?

I. Chromatium okenii

II. Nitrosomonas

III. Pseudomonas pseudoflava

a) I, III

b) I, II

c) I

d) II, III

Q.7. Match the following bacteria with their correct classification:

 a) i-A, ii-D, iii-C, iv-B

b) i-D, ii-C, iii-A, iv-B

c) i-D, ii-A, iii-B, iv-C

d) i-B, ii-D, iii-A, iv-C

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ANSWERS

1-a

2-c

3-b

4-b

5-b

6-c

7-d

REFERENCE

Black JG. Microbiology: principles and explorations.

The post Classification and Characteristics of Bacteria, Lectures on Bacteria Cell for BSc, MSc, B.Pharma appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.

Introduction

• A stain is a chemical which can bind with the cellular components and give them color. Different dyes which can be used for staining are basic/cationic dyes (methylene blue, crystal violet, malachite green, safranin) and anioninc/acidic dyes (eosin and picric acid).
• Cationic dyes bids with the negatively charged cellular components such as those are present in cell membrane, whereas, anionic dye binds with positively charged cellular components. [1]

Simple staining

Simple staining is the use of single dye which helps in revealing the basic cell shapes and cell arrangements. Stains which can be used in the simple staining are crystal violet, carbolfuchsin, safranin and methylene blue.

Differential staining

It is the use of two or more dyes to differentiate between two different kinds of organisms or two different parts of organisms. Two common methods for differential staining are:

• The gram staining
• The acid fast staining

The gram staining

Gram staining is based on the amount of peptidoglycan present in the cell wall of bacteria.

• Those bacteria which have thick layer of peptidoglycan in their cell wall are can retain the primary stain and are known as gram-positive bacteria.
• Those bacteria which have thin layer of peptidoglycan in their cell wall cannot retain the primary stain and are called gram-negative bacteria.

Steps for gram staining:

i. Bacterial smear is prepared on a slide.

ii. Crystal violet stain is added on the smear.

iii. After 1 min. stain is drains and rinsed with water and iodine mordant is added on the smear.

iv. After 1 min. iodine is drained and slide is rinsed with water.

v. Decolorizing with the help of alcohol and rinsing immediately

vi. Safranin is added, remains there for 1 min. and then drained and rinsed.

vii. Slide is looked under compound microscope.

Result interpretations:

Gram positive bacteria appear purple in color, whereas, gram negative bacteria retains the color red(pink) color of safranin dye.

The Ziehl-Neelsen acid fast staining

Tuberculosis and leprosy causing pathogens can be stained with the help of this technique. Organisms of genus Mycobacterium can be stained by acid-fast staining method. The lipid component in the acid fast bacteria is responsible for this property.

Steps:

i. Bacterial smear is prepared on a slide.

ii. Carbolfuchsin is added on the smear and heated

iii. After draining and rinsing, it is decolorized using 3% HCl in 95% ethanol and rinsed again.

iv. It is then stained with methyene blue dye.

Result interpretation:

Those bacteria belonging to the genus Mycobacterim will only retain the bright red color. Others will lose the red carbolfuchisin color.

MCQs

1. An example of cationic dye is?

a. Malachite green

b. Eosin

c. Picric acid

d. All of the above

2. Simple staining is used for?

a. Studying cellular organelles

b. Revealing basic cell shapes

c. Differentiating two different types of cell

d. Understanding the working of mitochondria

3. Gram staining is the type of?

a. Simple staining

b. Differential staining

c. Acid-fast staining

d. Special staining

4. Gram staining is based on?

a. Amount of lipid present in cell wall

b. Porosity of cell membrane

c. Amount of peptidoglycan present in cell wall

d. Type of flagella bacteria has

5. Correct steps for gram staining can be?

I. Addition of iodine mordant

II. Addition of crystal violet

III. Addition of safranin

IV. Decolorization with alcohol

II – I – IV – III

III – I – IV – II

II – IV – I – III

III – IV- I – II

6. Type of dyes used in the Ziehl-Neelsen acid fast staining?

I. Crystal violet

II. Carbolfuchsin

III. Safranin

IV. Methylene blue

a. I, II

b. I, III

c. II, III

d. II, IV

7. Match the following types of staining with their correct applications-

a. i-C, ii-B, iii-A

b. i-B, ii-C, iii-A

c. i-B, ii-A, iii-C

d. i-A, ii-B, iii-C

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ANSWERS

1-a

2-b

3-b

4-c

5-a

6-d

7-b

REFERENCES

The post STAINING Principle, Reagents, Procedure, Steps, Results Interpretation of gram staining and acid fast staining appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.

Phenindamine           

IUPAC nomenclature

2-methyl-9-phenyl-2,3,4,9-tetrahydro-1H-indeno[2,1-c]pyridine

Classification

• H1-receptor antihistamine
• Alkylamine antihistamine

Physiochemical Properties

Mechanism of Action

1. Phenindamine competes with histamine for binding with H1 receptor site on the effector cell.
2. Thus, all those pharmacological responses which were mediated by histamine at H1-receptor site are reduced and the intensity of allergic reactions and tissue injury response involving histamine release are reduced.

Structure Activity Relationship

Structure activity of alkyl amines antihistamines can be summarized as:

• E- and Z- isomers in alkenes shows large difference in activity, where, E-isomers are more potent than Z-isomers.
• The two aromatic rings have different binding environments at the receptors.
• 5-6 angstrom distance is required between aromatic ring and tertiary aliphatic amine for biding at the receptor.
• S­-enantiomers have greater affinity for H1 histamine receptors [1]

Method of synthesis

1. Acetophenone, methylamine and formaldehyde are reacted together to get ß,ß’-(methylamino)bis-(propiophenone).
2. The above formed compound is treated with sodium hydroxide to get 3-benzoyl-4-hydroxy-1-methyl-4-phenyl-piperidine.
3. On reaction of last with concentrated hydrogen bromide, 2-methyl-9-phenyl-2,3-dihydro-1H-indeno[2,1-c]pyridine is formed.
4. The last is reduced to get phenindamine. [2]

Medicinal Uses

Phenindamine is used for treatment of:

• Allergies
• Hay fever
• Common cold
• Watery eyes
• Runny nose
• Sneezing

Side Effects

Side effects of Phenindamine are:

• Fatigue
• Dizziness
• Drowsiness
• Sleepiness
• Dry mouth
• Enlarged prostate
• Difficulty in urination
• Headache
• Difficulty breathing
• Closing of throat
• Swellings in face

MCQs

Q.1 Match the following with correct SAR of the alkylamines antihistamine drugs:

1. i-A, ii-C
2. i-A, ii-D
3. i-B, ii-C
4. i-B, ii-D

Q.2 Correct sequence for the True/False for correct IUPAC names of the drug can be?

• Phenindamine: 2-methyl-9-phenyl-2,3,4,9-tetrahydro-1H-indeno[2,1-c]pyridine
•  Diphenhydramine: 2-(diphenylmethoxy)-N,N-dimethylethanamine
•  Auranofin: gold(1+);3,4,5-triacetyloxy-6-(acetyloxymethyl)oxane-2-thiolate;triethylphosphanium
•  Meloxicam: 4-hydroxy-2-methyl-N-(5-methyl-1,3-thiazol-2-yl)-1,1-dioxo-1λ6,2-benzothiazine-3-carboxamide

a) TFFT

b) FFTF

c) TTTT

d) FFFT

Q.3 Molecular weight of Phenindamine is?

a) 200.5 gm/mol

b) 540.6 gm/mol

c) 261.4 gm/mol

d) 1042 gm/mol

Q.4 Phenindamine binds with which receptor to produce antihistaminic actions?

a) α-receptors

b) ß-receptors

c) Nicotinic receptor

d) H1-receptor

Q.5 Which amongst the following is not a therapeutic use of drug phenindamine?

a) Runny nose

b) Sneezing

c) Hay fever

d) Hypertension

Q.6 Which of the following drug and their classification are correct?

I. Phenindamine: H1 receptor antihistamine drug

II. Cimetidine: H2 receptor antihistamine drug

III. Lansoprazole: Proton pump inhibitor

IV. Thiotepa: Antineoplastic drug

a) I, III

b) I, II, III, IV

c) III, IV

d) I, II, IV

Q.7 Number of chiral centers present in the structure of phenindamine is?

a) 0

b) 1

c) 2

d) 3

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ANSWERS

1-a

2-c

3-c

4-d

5-d

6-b

7-b

REFERENCES

The post PHENINDAMINE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.

IUPAC nomenclature

1-benzhydryl-4-methyl-piperazine

Classification

• H1-receptor antihistamine
• Piperazine antihistamine

Physiochemical Properties

Mechanism of Action

• Cyclizine blocks the action of histamine on the receptors present at vomiting center (CTZ).
• Cyclizine also have anti-cholinergic properties, thus, it also blocks muscarinic receptors.

Structure Activity Relationship

Structure activity of piperizine antihistamines can be summarized as:

• These are the derivatives of ethylene diamines.
• The connecting moiety is CHN group
• Primary structural difference is nature of para aromatic ring substituent
• These are moderately potent.
• Slow onset of action
• Low incidence of drowsiness
• They also exhibit peripheral and central antimuscarinic activity.

Method of synthesis

Alkylation of 1-methylpiperazine with benzhydrylbromide gives cyclizine. [1]

Medicinal Uses

Cyclizine is used for treatment of:

• Nausea
• Vomiting
• Dizziness
• Motion sickness

Side Effects

Side effects of cyclizine are:

• Difficult in urination
• Pounding heartbeats
• Lightheadedness
• Drowsiness
• Weakness
• Loss of coordination
• Nausea
• Dry mouth
• Constipation
• Blurred vision
• Difficult breathing
• Signs of allergic recations
• Swellings

MCQs

Q.1 Correct statements from the following related with the physicochemical properties of drug cyclizine are?

I. Molecular weight: 266.4 gm/mol

II. Appearance: White or creamy white crystalline powder

III. Melting Point: 105.5^oC

IV. Solubility: Soluble in alcohol

a) I, II, IV

b) I, III, IV

c) II, IV

d) I, II, III, IV

Q.2 Match the following of the drugs with their correct IUPAC names.

a) i-D, ii-B, iii-C, iv-A

b) i-A, ii-B, iii-D, iv-C

c) i-B, ii-C, iii-A, iv-D

d) i-A, ii-C, iii-D, iv-B

Q.3 Cyclizine has actions on?

I. Vomiting center

II. Cholinergic receptors

III. Muscarinic receptors

IV. Nicotinic receptors

a) I, III

b) I, IV

c) I, II, III

d) I

Q.4 Correct sequence for True/false for the classification of the drug can be?

• Cyclizine: H1-receptor antihistamine drug
• Haloperidol: Inhalational anesthetics
• Codeine: Narcotic analgesic
• Triclofos sodium: Sedative-hypnotics

a) TFTF

b) TTTT

c) FFTF

d) TFFT

Q.5 Piperizine antihistamine drugs are derivatives of?

a) Ethylene diamine

b) Piperidine

c) Benzodiazepine

d) Phenothiazine

Q.6 Type of rings present in the structure of cyclizine?

I. Pyridine

II. Piperazine

III. Phenyl

IV. Benzodiazepine

a) I, IV

b) I

c) II, III

d) II 

Q.7 Side effect of drug Cyclizine is/are?

a) Difficulty urination

b) Loss of coordination

c) Nausea

d) All of the above

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ANSWERS

1-d

2-a

3-c

4-b

5-a

6-c

7-d

REFERENCES

[1] Vardanyan R, Hruby V. Synthesis of essential drugs. Elsevier; 2006 Mar 10.

The post CYCLIZINE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.

IUPAC nomenclature

1-[(4-Chlorophenyl)(phenyl)methyl]-4-methylpiperazine

Classification

• H1-receptor antihistamine
• Piperazine antihistamine

Physiochemical Properties

Mechanism of Action

Antihistamines such as chlorcyclizine acts as pharmacological antagonists of hitamine at the histamine receptor sites. They do not prevent the release of histamine.

There is also hepatic microsomal enzyme-inducing properties of chlorcyclizine which results in shortening of duration of action of some barbiturates as result of enzyme induction.

Structure Activity Relationship

Structure activity of piperizine antihistamines can be summarized as:

• These are the derivatives of ethylene diamines.
• The connecting moiety is CHN group
• Primary structural difference is nature of para aromatic ring substituent
• These are moderately potent.
• Slow onset of action
• Low incidence of drowsiness
• They also exhibit peripheral and central antimuscarinic activity.

Method of synthesis

Alkylation of 1-methylpiperazine with 4-chlorobenzhydrylbromide gives chlorcyclizine. [1]

Medicinal Uses

Chlorcyclizine has:

• Mildly sedative properties
• Antihistaminic properties
• Slight anticholinergic properties
• Antispasmodic properties
• It enhances the action of epinephrine
• Local anesthetic action

Side Effects

Side effects of chlorcyclizine are:

• Sedation
• Dizziness
• Tinnitus
• Lassitude
• Loss of coordination
• Fatigue
• Blurred vision
• Diplopia
• Euphoria
• Nervousness
• Insomnia
• Tremors 

MCQs

Q.1 Mechanism of action of chlorcyclizine drug includes?

a) Release of histamine in prevented

b) Release of histamine is stimulated

c) Antagonistic effects at H1 receptor for histamine

d) Agonist effects H1 receptor for Histamine

Q.2 Therapeutic use of drug Chlorcyclizine is/are?

a) Local anesthetic

b) Sedative

c) Antihistamine

d) All of the above

Q.3 The type of ring present in the structure of chlorcyclizine?

a) Piperazine

b) Pyridine

c) Cyclohexane

d) All of the above

Q.4 Number of chiral carbons present in the structure of Chlorcyclizine?

a) 0

b) 1

c) 2

d) 3

Q.5 Correct sequence for the True/False for the physiochemical properties of the drug Chlorcyclizine can be?

• Molecular weight: 300.8 gm/mol
• Physical appearance: Oil
• Octanol/water partition coefficient: 3.45

a) TTT

b) TFT

c) FFT

d) TFF

Q.6 Correct statements for the IUPAC nomenclatures of the drugs are?

I. Chlorcyclizine: 1-[(4-Chlorophenyl)(phenyl)methyl]-4-methylpiperazine

II. Carbinoxamine: 2-[(4-Chlorophenyl)-pyridin-2-yl-methoxy]-N,N-dimethyl-ethanamine

III. Edrophonium: Ethyl-(3-hydroxyphenyl)-dimethylazanium

IV. Tenoxicam: 4-hydroxy-2-methyl-1,1-dioxo-N-pyridin-2-ylthieno[2,3-e]thiazine-3-carboxamide

a) I, II

b) III, IV

c) IV

d) I, II, III, IV

 Q.7 Match the following drugs with their correct classifications-

 a) i-A, ii-C, iii-D, iv-B

b) i-D, ii-A, iii-C, iv-B

c) i-D, ii-B, iii-A, iv-C

d) i-B, ii-D, iii-A, iv-C

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ANSWERS

1-c

2-d

3-d

4-b

5-a

6-d

7-b

REFERENCES

[1] US 2 630 435 (Burroughs Wellcome; 1953; prior. 1948).

The post CHLORCYCLIZINE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.

IUPAC nomenclature

1-[(4-chlorophenyl)-phenylmethyl]-4-[(3-methylphenyl)methyl]piperazine

Classification

• H1-receptor antihistamine
• Piperazine antihistamine

Physiochemical Properties

Mechanism of Action

• Meclizine inhibits the signal transmission from the vestibular nuclei and NTS (nucleus of solitary tract) to the vomiting center and hemoreceptor trigger zone (CTZ) through antagonistic effects on H1 receptors.
• It also decreases the vestibular stimulation and labyrinth excitability.

Structure Activity Relationship

Structure activity of piperizine antihistamines can be summarized as:

• These are the derivatives of ethylene diamines.
• The connecting moiety is CHN group
• Primary structural difference is nature of para aromatic ring substituent
• These are moderately potent.
• Slow onset of action
• Low incidence of drowsiness
• They also exhibit peripheral and central antimuscarinic activity.

Method of synthesis

Reductive deamination of 3-methylbenzaldehyde with 1-(4-chlorbenzhydryl)piperazine using hydrogen over Raney nickel produces meclizine. [1]

Medicinal Uses

Meclizine is used for treatment of:

• Nausea
• Vomiting
• Dizziness
• Motion sickness
• Symptoms of vertigo

Side Effects

Side effects of Meclizine are:

• Drowsiness
• Vomiting
• Dry mouth
• Fatigue
• Headache
• Difficulty in breathing
• Swelling of face

MCQs

Q.1 “1-[(4-chlorophenyl)-phenylmethyl]-4-[(3-methylphenyl)methyl]piperazine” is the IUPAC nomenclature of which drug?

a) Loperamide

b) Meclizine

c) Buclizine

d) Lansoprazol

Q.2 Melting point of meclizine is?

a) 520^oC

b) 217-224^oC

c) 120^oC

d) 25^oC

Q.3 Match the following with correct classifications of the drugs.

a) i-A, ii-D, iii-C, iv-B

b) i-D, ii-C, iii-A, iv-B

c) i-D, ii-A, iii-B, iv-C

d) i-B, ii-D, iii-A, iv-C

Q.4 Mechanism of action of Meclizine includes?

I. Antagonistic effects on H1-receptor.

II. Decrease in the vestibular stimulation and labyrinth excitability.

III. Inhibition of Hydrogen/Potassium pump

IV. Inhibition of COX-2 enzyme

a) I, II

b) II, IV

c) I, II, III

d) III

Q.5   Correct sequence for True and False for the given statements related with the SAR of Piperazine antihistamines can be?

• These are the derivatives of ethylene diamines.
• The connecting moiety is CHN group
• Primary structural difference is nature of para aromatic ring substituent
• These are moderately potent

a) TTFT

b) TFTF

c) TTTT

d) FTTT

Q.6 Reductive deamination of 3-methylbenzaldehyde with 1-(4-chlorbenzhydryl)piperazine using hydrogen over Raney nickel produces which drug?

a) Methotrexate

b) Omeprazol

c) Meclizine

d) Carbinoxamine

 Q.7 The drug Meclizine is mainly used for treatment of?

a) Nausea

b) Dizziness

c) Symptoms of vertigo

d) All of the above

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ANSWERS

1-b

2-b

3-c

4-b

5-c

6-c

7-d

REFERENCES

[1] Vardanyan R, Hruby V. Synthesis of essential drugs. Elsevier; 2006 Mar 10.

The post MECLIZINE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.

IUPAC nomenclature

(RS)-1-[(4-chlorophenyl)- phenyl-methyl]-4- [(4-tert-butylphenyl) methyl] piperazine

Classification

• H1-receptor antihistamine
• Piperazine antihistamine

Physiochemical Properties

Mechanism of Action

• Buclizine blocks the action of histamine on the receptors present at vomiting center (CTZ).
• Buclizine also have anti-cholinergic properties, thus, it also blocks muscarinic receptors.

Structure Activity Relationship

Structure activity of piperizine antihistamines can be summarized as:

• These are the derivatives of ethylene diamines.
• The connecting moiety is CHN group
• Primary structural difference is nature of para aromatic ring substituent
• These are moderately potent.
• Slow onset of action
• Low incidence of drowsiness
• They also exhibit peripheral and central antimuscarinic activity.

Method of synthesis

i. 4-chlorobenzhydryl chloride is reacted with ethyl piperazine N-carboxylate to give ethyl-4-(4-chlorobenzhydryl)piperazine-1-carboxylate.

ii. The above formed compound is treated with NaOH to get 1-(4-chlorobenzhydryl)piperazine.

iii. The last is reacted with 4-tert-butyybenzyl chloride to get Buclizine. [1]

Medicinal Uses

Buclizine is used for treatment of:

• Nausea
• Vomiting
• Dizziness
• Motion sickness

Side Effects

Side effects of Buclizine are:

• Drowsiness
• Vomiting
• Dry mouth
• Fatigue
• Headache
• Difficulty in breathing
• Swelling of face

MCQs

Q.1 What can be the correct IUPAC nomenclature of Buclizine?

a) (RS)-1-[(4-chlorophenyl)- phenyl-methyl]-4- [(4-tert-butylphenyl) methyl] pyrimidine

b) (R)-(+)-2-([3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methylsulfinyl)-1H-benzo[d]imidazole

c) (RS)-1-[(4-chlorophenyl)- phenyl-methyl]-4- [(4-tert-butylphenyl) methyl] piperazine

d) (R)-(+)-2-([3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methylsulfinyl)-imidazole

Q.2 Which amongst the following statements is/are incorrect related to the SAR of Piperazine antihistamines?

I. These are the derivatives of Ehanol.

II. The connecting moiety is CHN group

III. Primary structural difference is nature of para aromatic ring substituent

a) I

b) II, III

c) I, III

d) I, II, III

Q.3 Types of rings present in the structure of Buclizine?

I. Piperazine

II. Pyridine

III. Pyrolle

IV. Phenyl

a) I, III

b) I, IV

c) II, IV

d) II, III

Q.4 Side effects of drug Buclizine is/are?

a) Drowsiness

b) Vomitting

c) Headache

d) All of the above

Q.5 Match the following drugs with their correct molecular weight-

 a) i-A, ii-B, iii-C, iv-D

b) i-C, ii-A, iii-B, iv-D

c) i-C, ii-D, iii-A, iv-B

d) i-A, ii-C, iii-D, iv-B

Q.6 An example of drug from class piperazine antihistamine drug?

a) Buclizine

b) Cimetidine

c) Glycopyrrolate

d) All of the above 

Q.7 Octanol/water partition coefficient of Buclizine is?

a) 2.5

b) 3.2

c) 4.8

d) 7.1

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ANSWERS

1-c

2-a

3-b

4-d

5-c

6-a

7-d

REFERENCES

[1] DE 964 048 (H. Morren; appl. 1952; B-prior. 1951).

The post BUCLIZINE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.