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Questions and Answers

The following statement is/are true regarding the relationship of bond length and bond polarity except: . As the bond polarity increase, the bond length decreases b. A C-F bond has a longer bond length than C-C c. As bond polarity increases the bond length also increases d. A and B only e. B and C only

  • A) A C-F bond has a longer bond length than C-C
  • B) As bond polarity increases the bond length also increases
  • C) A and B only
  • D) As the bond polarity increase, the bond length decreases (correct)
  • E) B and C only
  • The following statement/s is/are true regarding the relationship of hybridization of orbitals and bond length: a. As the s character increases, the bond length increases b. As the s character increases, the bond length decreases c. The bond length of acetylene is longer than the bond length of ethylene d. The bond length of ethane is shorter than the bond length of ethylene e. None of the choices

  • The bond length of ethane is shorter than the bond length of ethylene
  • As the s character increases, the bond length increases
  • As the s character increases, the bond length decreases (correct)
  • The bond length of acetylene is longer than the bond length of ethylene
  • None of the choices
  • Bond strength or bond energy is the energy necessary to break the only bond in a diatomic molecule or to dissociate the bonded atoms to their bond state. Which of the following statements is/are true regarding its relationship with orbital hybridization, bond length and bond poarity?

  • A) When the polarity of the bond increases, the bond energy also increases
  • B) All of the choices (correct)
  • C) When the s character of the bonding orbitals increases, the bond energy also increases
  • D) Bond energy and bond length has inverse relationship.
  • E) A and B only
  • What is the name of the following structure: CH3CH2CH2-C=CH

    <p>E) A and B (@)</p> Signup and view all the answers

    Organic pharmaceuticals are often complex molecules which have a variety of acidic and basic functional groups. The behaviour of these groups in an aqueous environment will influence the activity of the drug and its absorption in the different compartments of the body. Which of the following statement is/are true regarding the pH of the medium and the acidic/basic property of the drug?

    <p>All of the above (@)</p> Signup and view all the answers

    Which of the following statements is/are true regarding drug distribution and pKa?

    <p>E) A and B only (@)</p> Signup and view all the answers

    These lipid soluble compounds are also paraffin or saturated hydrocarbons. They commonly undergo halogination and combustion reaction and, in vivo, terminal carbon or side chain hydroxylation may occur.

    <p>Alkanes (A)</p> Signup and view all the answers

    These lipid soluble compounds are also known as olefins and unsaturated hydrocarbons. Their common reactions are the addition of hydrogen or halogenation, hydration (to form glycols), and oxidation (to form peroxides).

    <p>Alkenes (B)</p> Signup and view all the answers

    The structure of these compounds is based on benzene. These molecules exhibit multicenter bonding, which confers unique chemical properties.

    <p>Aromatic hydrocarbon (C)</p> Signup and view all the answers

    Which of the following alcohols is the most water soluble?

    <p>Methanol (A)</p> Signup and view all the answers

    Which of the following statement is /are true regarding oxidation of alcohols?

    <p>D) Tertiary alcohols ordinarily are not oxidized (C)</p> Signup and view all the answers

    Which of the following compounds has a general formula of R-O-R with an oxygen bonded to 2 carbon atoms?

    <p>Ether (B)</p> Signup and view all the answers

    These compounds have a general formula of R-CHO and contain a carbon group (C=O). The common reactions of these compounds are oxidation and hemiacetal and acetal formation.

    <p>Aldehydes (A)</p> Signup and view all the answers

    Which of the following statements is/are correct about the water solubility of amines?

    <p>E) A and C only (@)</p> Signup and view all the answers

    These compounds have a general formula of RCOOR and commonly undergo hydrolysis to form carboxylic acid and alcohol.

    <p>Esters (C)</p> Signup and view all the answers

    These compounds have a general formula of RCOOH and commonly undergo salt formation with bases, esterification and decaroxylation.

    <p>Carboxylic acid (@)</p> Signup and view all the answers

    Which of the following functional group when added to a benzene nucleus, decreases the lipid solubility of the benzene

    I. A carboxylic acid group II. An ethyl group III. A phenolic group

    <p>I and III are correct (@)</p> Signup and view all the answers

    Decomposition the drug molecule at room temperature most likely would occur by

    <p>A) Hydrolysis of the ester (A)</p> Signup and view all the answers

    Reactions that will be possible metabolic pathways for the drug molecule include

    I. Ring hydroxylation II. Glucuronide formation III. Enzymatic hydrolysis

    <p>I, II, III are correct (C)</p> Signup and view all the answers

    Which of the following statements is/are true regarding drugs?

    <p>All of the above (@)</p> Signup and view all the answers

    Most drugs bind to their targets by means of intermolecular bonds. Which of the following statements is/are true regarding these forces?

    <p>E) A and C only (@)</p> Signup and view all the answers

    This is the type of enzyme inhibition where the drug react with the enzyme and forms a covalent bond.

    <p>Irreversible inhibition (B)</p> Signup and view all the answers

    These type of inhibitor binds to the enzyme substrate complex in which its effect cannot be overcome by increasing the substrate concentration

    <p>Uncompetitive inhibitor (D)</p> Signup and view all the answers

    Which of the following drugs is incorrectly match with its target enzyme?

    <p>5-flourouracil: Bactericidal topoisomerase (D)</p> Signup and view all the answers

    This type of inhibitor binds to a binding site different from the active site. They alter the shape of the enzyme such that the active site is no longer recognizable.

    <p>Allosteric inhibitor (@)</p> Signup and view all the answers

    Evaluate the following statements: Antagonists can mimic the natural messengers and activate receptors. Antagonist can bind to the receptor but they do not activate it.

    <p>Only the second statement is correct. (D)</p> Signup and view all the answers

    The following factors must be considered in designing an agonist:

    <p>E) All of the above (@)</p> Signup and view all the answers

    Which of the following statements is/are true regarding structurally-specific and structurally non specific drugs?

    I. The biologic effect of structurally non specific drugs is more closely correlated with the physical properties of the molecules than with the chemical structure. II. Examples of structurally non specific drugs are 6-mercaptopurine, phenothiazines, pyrimethamine, and primaquine. III. The biologic effect of structurally specific drugs, although not completely independent of the physical properties, depends on certain chemical structure on drug molecule. Chemical reactivity of the drug plays an important role as reflected in bonding propensities and exactness of fit on the receptors. IV. General anesthetics, hypnotics and volatile insecticides are typical examples of structurally specific drugs.

    <p>I and III is correct (@)</p> Signup and view all the answers

    Which of the following drug-enzyme pairs is/are correctly matched?

    I. Penicillins – transpeptidase II. Cephalosphorins – transpeptidase III. Pyrimethamine – Dihydrofolate reductase IV. Epinephrine – Adenylyl cyclise

    <p>I, II, and IV are correct (D)</p> Signup and view all the answers

    It is generally conceived that an exact fit of the drug molecule and receptor is necessary to evoke maximal biologic response that is imperative to consider the stereochemical makeup of drugs. Which of the following statements is/are true regarding the biologic activity of some stereochemical isomers?

    I. Only the (-) isomer of ascorbic acid has antiscorbutic activity
    II. Only the D isomers of alpha and beta glucose show high affinity for the red blood cell sugar transfer stem. III. Only the (-) isomer of alpha methyldopa has hypotensive activity IV. Only the D(threo) isomer has high anti-bacterial activity

    <p>I, II, III, and IV are correct (@)</p> Signup and view all the answers

    What is the rate-limiting step in drug absorption of orally administered solid dosage forms?

    <p>B) Dissolution rate (A)</p> Signup and view all the answers

    Which of the following factors can influence the dissolution rate of drugs from solid dosage forms and hence, the therapeutic activity?

    I. Solubility, particle size, crystalline form and salt form of the drug II. Rate of disintegration in the gastrointestinal lumen III. Gastric pH, motility and presence of food at the absorption site

    <p>I, II, and III are correct (C)</p> Signup and view all the answers

    Which of the following statements is/are true regarding renal excretion of drugs?

    I. Renal excretion involves three processes: glomerular filtration, secretion and tubular reabsorption. II. Both the free drug and the drug bond to plasma proteins are filtered by the kidneys. III. Drugs with high lipid/water partition coefficients are reabsorbed readily while those with low lipid/water partition coefficients are unable to diffuse back across the tubular membrane and are excreted in the urine unless reabsorbed by an active carrier system. IV. Altering the pH of urine can result to termination of biologic activity of weakly acidic and basic drugs

    <p>. I, III, and IV are correct (C)</p> Signup and view all the answers

    Which of the following statements is/are true regarding Phase I and Phase II Metabolic reactions?

    I. Phase I reactions include oxidation, hydroxylation, reduction and hydrolysis-enzymatic reactions in which a new functional group in introduced into the drug molecule or an existing functional group is modified making the drug more polar and more readily excreted. II. Phase II reactions are enzymatic syntheses whereby a functional group is masked by the addition of a new group, for example, acetyl, sulphate, glucoronic acid or certain amino acids, which increases the polarity of the drug. III. Most drugs undergo phase I reactions only. IV. Drugs that are resistant to drug-metabolizing enzymes or that are hydrophilic are excreted largely unchanged.

    <p>. I, II, and IV are correct (D)</p> Signup and view all the answers

    Which of the following statements regarding NADPH-Dependent Oxidative Reactions in Liver Microsomes is/are correct? I. Aniline is converted to p-Aminophenol by aromatic hydroxylation II. Codeine is converted to morphine and formaldehyde by N-dealkylation. III. Imipramine is converted to Despiramine by O-dealkylation IV. Amphetamine is converted to Phenylacetone by deamination

    I. Aniline is converted to p-Aminophenol by aromatic hydroxylation II. Codeine is converted to morphine and formaldehyde by N-dealkylation. III. Imipramine is converted to Despiramine by O-dealkylation IV. Amphetamine is converted to Phenylacetone by deamination

    <p>I and IV are correct (C)</p> Signup and view all the answers

    Phase I metabolic transformation introduce new and polar functional groups into the molecule, which may produce one or more of the following changes, except:

    <p>None of the choices (@)</p> Signup and view all the answers

    Which of the following Phase II pathway is correctly paired with their activated conjugating immediate?

    I. Glucoronic acid conjugation: uridine phosphate glucoronic acid (UDP-GA) II. Sulfate conjugation: 3’-phospho adenosine-5’-phosphosulfate (PAPS) III. Methylation: S-adenosylmethionine IV. Amide synthesis: Coenzyme A

    <p>I, II, III, and IV are correct (@)</p> Signup and view all the answers

    Sulfonamides can undergo which metabolic pathway?

    I. Acetylation at the N4 amino group II. Conjugation with glucoronic acid or sulphate at the N4 amino group III. Acetylation or conjugation with glucoronic acid at the N1 amino group
    IV. Hydroxylation and conjugation in the heterocyclic ring, R

    <p>I, II, III, and IV are correct (@)</p> Signup and view all the answers

    The first purely synthetic antimicrobial drug which was developed by Paul Erlich. This drug was used in the treatment of tryponosomiasis and syphilis.

    <p>Salvarsan (B)</p> Signup and view all the answers

    Which of the following antibacterial agents acts by inhibiting the metabolism of microbial organism but not of the host?

    <p>Sulfonamides (A)</p> Signup and view all the answers

    Which of the following antibacterial agents inhibit s bacterial cell wall synthesis?

    <p>Penicillins (B)</p> Signup and view all the answers

    Which of the following antibacterial agent can interact with the plasma membrane of bacterial cells to affect membrane permeability?

    <p>Polymyxins (B)</p> Signup and view all the answers

    Which of the following antibacterial agents can disrupt the synthesis of essential proteins and enzyme required for the cell’s survival?

    <p>Rifamycin (D)</p> Signup and view all the answers

    This antibacterial agent can inhibit the nucleic acid transcription and replication which prevents cell division and.or protein synthesis.

    <p>Nalidixic acid (@)</p> Signup and view all the answers

    Which of the following statements is/are correct regarding the structure-activity relationship of sulphonamides?

    I. The p-amino group must be unsubstituted unless it is a prodrug or when the body can further metabolize it to generate the active compound. II. Extra substitution of the aromatic ring increases activity. III. The sulphonamide nitrogen must be primary or secondary.

    <p>I and III only (B)</p> Signup and view all the answers

    Which part of the drug molecule can only be varied to retain the antibacterial activity?

    <p>C) R2 (C)</p> Signup and view all the answers

    A sulphonamide used in combination with pyrimethamine in the treatment of Malaria.

    <p>Sulfadoxine (C)</p> Signup and view all the answers

    It is an orally active dyaminopyridine structure which has proved to be highly selective antibacterial and antimalarial agent often given in conjunction with sulfamethoxazole. It inhibits the enzyme dihydrofolate reductase leading to the inhibition of DNA synthesis and cell growth.

    <p>Trimethoprim (B)</p> Signup and view all the answers

    Successfully isolated penicillin using processes such as freeze-drying and chromatography.

    <p>Florey and Chain (B)</p> Signup and view all the answers

    Addition of electron-withdrawing group into the acyl side chain of penicillin structure will render the drug

    <p>resistant to acid hydrolysis (A)</p> Signup and view all the answers

    What is the effect of steric shields to the penicillin structure?

    <p>It will be protected from B-lactamase enzymes (B)</p> Signup and view all the answers

    This drug is a penicillin analogue with isoxazolyl incorporated in the acyl side chain making it useful against Staphylococcus aureus infections and acid resistant.

    <p>Flucloxacillin (A)</p> Signup and view all the answers

    Which of the following broad-spectrum penicillin analogues do not have a urea functional group at the alpha-position?

    <p>Ticarcillin (C)</p> Signup and view all the answers

    Which of the following broad spectrum penicillin analogues has carboxylic acid group in the acyl side chain?

    <p>Ticarcillin (C)</p> Signup and view all the answers

    Which of the following amino acids are the biosynthetic precursors of penicillin?

    <p>E) B and C only (@)</p> Signup and view all the answers

    Which of the following statements is incorrect regarding the chemical structure of cephalosporins?

    <p>B) The B-lactam ring of cephalosporins is fused to five-membered dihydrothiazine ring. (B)</p> Signup and view all the answers

    Which of the following statements correctly describe/s the structure of carbapenems such as imipenem and meropenem?

    <p>D) A and B only (D)</p> Signup and view all the answers

    Clavulanic acid is a beta-lactamase inhibitor used in combination with amoxicillin and other Blactamase antibiotics. Which of the following statements correctly describe clavulanic acid?

    <p>D) A and B only (D)</p> Signup and view all the answers

    Clavulanic acid, Sulbactam and tazobactam are B-lactamase inhibitors that act as suicide substrates are administered with B-lactam antibiotics to prevent their degradation. Which of the following combinations are correctly matched to their brand names?

    <p>C) Clavulanic acid + amoxicillin = Augmentin (C)</p> Signup and view all the answers

    This antibiotic was isolated from Streptomyces garyphalus and inhibits bacterial cell wall synthesis by mimicking the structure of D-Alanine and inhibiting the enzymes L-Alanine racemase and D-Ala-D-Ala ligase.

    <p>D-cycloserine (C)</p> Signup and view all the answers

    A polypeptide complex produced from Bacillus subtilis that binds and inhibits the carrier lipid responsible for carrying the cell wall components across the cell membrane.

    <p>Bacitracin (A)</p> Signup and view all the answers

    A glycopeptide antibiotic isolated from Streptomyces orientalis.

    <p>Vancomycin (B)</p> Signup and view all the answers

    A glycopeptide antibiotic isolated from Actinomyces teichomyceticus

    <p>Teicoplanin (@)</p> Signup and view all the answers

    An antibiotic composed of 16 amino acids that is described as a ‘tunnelling’ molecule that act on the plasma membrane and result in the uncontrolled movement of ions across cell membrane leading to cell death.

    <p>Gramicidin A (B)</p> Signup and view all the answers

    An ionophore antibiotic with a cyclic structure obtained from Streptomyces fermentation that acts on the plasma membrane structure by allowing the uncontrolled movement of ions across the cell membrane. This ionophore is specific for potassium ions over sodium ions.

    <p>Valinomycin (C)</p> Signup and view all the answers

    A polypeptide antibiotic derived from Bacillus polymyxa which can cause leakage of small molecules such as nucleosides from the cell resulting to cell death.

    <p>Polymyxin B (D)</p> Signup and view all the answers

    A cyclic lipopeptide derived from a bacterial strain of Streptomyces roseosporus and works by disrupting multiple functions of bacterial cell membrane.

    <p>Daptomycin (A)</p> Signup and view all the answers

    A bactericidal protein synthesis inhibitor that was isolated from Streptomyces griseus. This antibiotic contains a carbohydrate and basic amine groups in its structure.

    <p>Streptomycin (B)</p> Signup and view all the answers

    A bacteriostatic antibiotic which inhibits protein synthesis by binding to the 30s subunit of ribosomes and preventing aminoacyl tRNA from binding. This drug was isolated from Streptomyces aureofasciens.

    <p>Chlortetracycline (A)</p> Signup and view all the answers

    Which of the following antibiotics has a large lactone ring, a ketone group and a glycosidically linked amino sugar in its structure?

    <p>Erythromycin (@)</p> Signup and view all the answers

    Clindamycin, a sulphur containing antibiotic, must not be given with which of the following drugs because of having the same binding site at the ribosomes?

    <p>E) B and C only (@)</p> Signup and view all the answers

    Quinupristin and Dalfupristin are streptogramins isolated from

    <p>Streptomyces pristinaespiralis (B)</p> Signup and view all the answers

    Which of the following drug is an oxazolidinone that can prevent the formation of 70s ribosome by binding to the 50s subunit?

    <p>Linezolid (B)</p> Signup and view all the answers

    Nalidixic acid was the first therapeutically agent in the class of compounds that inhibits topoisomerase enzymes, resulting in inhibition of replication and transcription. Which of the following is related to nalidixic acid?

    <p>Ofloxacin (C)</p> Signup and view all the answers

    An aminoacridine agent used topically to treat deep surface wounds. It can interact directly with bacterial DNA by intercalation.

    <p>Proflavine (@)</p> Signup and view all the answers

    The antibiotic isolated from Streptomyces mediterranei which inhibits Gram positive bacteria and works by binding noncovalently to DNA-dependent RNA polymerase and inhibiting the start of RNA synthesis. The flat naphthalene ring and several of the hydroxyl groups in its structure are essential for activity, and the drug exists in as zwitterions giving it good solubility in both aqueous acid and lipids

    <p>. Rifamycin B (A)</p> Signup and view all the answers

    A nitroimidazole structure introduced as an anti-protozoal agent and later became anti bacterial agent. Its mechanism of action involves the drug entering the bacterial cell wall where the nitro group is reduced and free radicals are formed and act on DNA.

    <p>Metronidazole (C)</p> Signup and view all the answers

    A drug used to treat urinary tract infections where it degrades in acid conditions to give formaldehyde as the active agent.

    <p>Methenamine (B)</p> Signup and view all the answers

    An antiviral drug that has a nucleoside-like structure and contains the same nucleic acid base as deoxyguanosine, but lacks the complete sugar ring. It specifically inhibits viral DNA polymerase and used in the treatment of infections due to herpes simplex 1 and 2 as well as varicella-zoster viruses.

    <p>Acyclovir (A)</p> Signup and view all the answers

    Which of the following is the valine ester prodrug of acyclovir useful in the treatment of varicellazoster virus infections?

    <p>Valaciclovir (C)</p> Signup and view all the answers

    Which of the following antiviral drug is an analogue of deoxythymidine used in the treatment of herpes keratitis? The triphosphate form of this drug inhibits viral DNA polymerase as well as thymidylate synthetase.

    <p>Idoxuridine (B)</p> Signup and view all the answers

    A plant product used in the treatment of genital warts caused by DNA virus papilloma virus

    <p>Podophyllotoxin (C)</p> Signup and view all the answers

    This drug consists of 21 nucleotides and phosphothionate backbone. It is a DNA antisense molecule that blocks the translation of viral RNA and is used against retinal inflammation caused by CMV in AIDS patients.

    <p>Fomivirsen (D)</p> Signup and view all the answers

    A nucleoside reverse transcriptase inhibitor which is an analogue of deoxythymidine where the 3’hydroxyl group is replaced by an azido group.

    <p>Zidovudine (A)</p> Signup and view all the answers

    The anti-HIV drug contains inosine as the nucleic acid base and is converted through a series of enzyme reaction to 2’,3’-dideoxyadenosine triphosphate which is the active drug.

    <p>Didanosine (B)</p> Signup and view all the answers

    Which of the following anti-HIV drug is an analogue of deoxycytidine where the 3’ carbon has been replaced by sulphur?

    <p>Lamivudine (C)</p> Signup and view all the answers

    The only guanosine analogue that is used against HIV infections and Hepatitis B.

    <p>Abacavir (D)</p> Signup and view all the answers

    A second generation non-nucleoside reverse transcriptase inhibitor that has a benzoxaxinone structure.

    <p>Efavirenz (@)</p> Signup and view all the answers

    Which of the following statements is/are correct regarding anti-HIV drugs?

    <p>E) All of the above (@)</p> Signup and view all the answers

    Which substituent of chloramphenicol is responsibe for its toxic effect?

    <p>E) A and B only (@)</p> Signup and view all the answers

    Which of the following statements is correct regarding Erythromycin?

    I. Erythromycin binds to the 50s subunit of bacterial ribosomes II. When administered together with chloramphenicol, their bacteriostatic effect will increase. III. The ketone and 2 alcohol groups in its structure are responsible for its acid sensitivity. IV. Increasing the size of the macrocycle to a 16-membered ring can increase the acid stability of the molecule.

    <p>I, II, III, IV (A)</p> Signup and view all the answers

    Amantadine is one of the earliest antiviral drugs used clinically against flu. Which of the following statements is correct regarding amantadine?

    I. Amantadine is an adamantine related to rimantadine. II. It inhibits the penetration and uncoating of the influenza virus. III. It can inhibit replication of the influenza virus by blocking a viral ion channel called matrix (M2) protein IV. At high concentrations, it can alter pH of endosomes and prevent the acidic environment required by the hemagglutinins to fuse the viral membrane with that of the endosome.

    <p>I, II, III, IV (A)</p> Signup and view all the answers

    A semi-synthetic analogue of camptothecin given intravenously and is a prodrug used in combination with fluorouracil and folinic acid for the treatment of advanced colorectal cancer.

    <p>Irinotecan (D)</p> Signup and view all the answers

    An antisense drug designed to inhibit the mRNA molecules that code for proteins which suppress apoptosis.

    <p>Oblimersen (A)</p> Signup and view all the answers

    A natural product that reacts with nucleophiles to produce diradical species. Its reaction with DNA ultimately leads to cutting of the DNA chains.

    <p>Calicheamicin (B)</p> Signup and view all the answers

    It is the most commonly used alkylating agent in cancer chemotherapy, the metabolism of which produces arcolein which is toxic to the bladder and kidneys.

    <p>Cyclophosphamide (@)</p> Signup and view all the answers

    An alkylating agent that can cause intrastrand cross-linking preferref over cisplatin for the intravenous treatment of advanced ovarian tumors because of its less severe side effects.

    <p>Carboplatin (C)</p> Signup and view all the answers

    Which of the following drugs is not an alkylating agent used in cancer chemotherapy?

    <p>None of the choices (@)</p> Signup and view all the answers

    A thiopurine prodrug which is converted to its corresponding monophosphate that inhibits purine synthesis.

    <p>6-mercaptopurine (C)</p> Signup and view all the answers

    An antimetabolite that is very similar in structure to the natural folates differing only in additional amino and methyl groups. It inhibits the enzyme dihydrofolate reductase which is responsible in maintaining levels of the enzyme cofactor tetrahydrofolate.

    <p>Methotrexate (A)</p> Signup and view all the answers

    This drug acts as a prodrug for a suicide inhibitor. It is converted in the body to the fluorinated analogue of 2’deoxyuridylic acid monophosphate which then combines with the enzyme thymidylate synthase and the cofactor.

    <p>5-fluorouracil (B)</p> Signup and view all the answers

    An anti-leukemia drug isolated from Streptomyces antibioticus and is a powerful inhibitor of Adenosine deaminase.

    <p>Pentostatin (D)</p> Signup and view all the answers

    A prodrug analogue of 2’deoxycytidine which inhibits DNA polymerases

    <p>Cytarabine (@)</p> Signup and view all the answers

    Which of the following pairs is correctly matched?

    I. Glucocorticoids: Megestrol acetate II. Progestins: prednisone III. Estrogens: Diethylstilbestrol IV. Androgens: Fluoxymesterone

    <p>III, IV (C)</p> Signup and view all the answers

    A decapeptide analogue of the luteinizing hormone – releasing hormone designed to be more resistant to peptidase degradation.

    <p>Goserelin (A)</p> Signup and view all the answers

    A reversible competitive inhibitor of the enzyme aromatase , the design of which is based on structure of amino gluthetimide.

    <p>Anastrazole (D)</p> Signup and view all the answers

    This mode of therapy involves an antibody which has catalytic activity designed to activate a prodrug.

    <p>Antibody-directed abzyme prodrug therapy (ADAPT) (B)</p> Signup and view all the answers

    This mode of therapy involves the delivery of a gene that codes for an enzyme capable of activating an anticancer prodrug into a cancer cell.

    <p>Gene -directed enzyme prodrug therapy (GDEPT) (C)</p> Signup and view all the answers

    This involves irradiation of tumors containing porphyrin photosensitizers resulting to the production of reactive oxygen species which are fatal to the cell.

    <p>Photodynamic therapy (D)</p> Signup and view all the answers

    This therapy involves an antibody-enzyme conjugate that is targeted to specific cancer cells. Once the antibody has become attached to the outer surface of cancer cells, a prodrug is administered which is activated by the enzyme at the tumor site.

    <p>Antibody-directed enzyme prodrug therapy (ADEPT) (A)</p> Signup and view all the answers

    Which of the following statements is true regarding acetylcholine?

    I. It is very useful in treating such conditions that requires it because it can be readily synthesized in the laboratory. II. It is easily hydrolyzed in the stomach by acid catalysis and cannot be given orally. III. It is administered intravenously as it is stable in blood because of the absence of enzymes such as esterases. IV. There is no selectivity of action upon administration of acetylcholine.

    <p>II, IV (@)</p> Signup and view all the answers

    Which of the following statements is true regarding acetylcholine analogues?

    <p>D) A and B (D)</p> Signup and view all the answers

    Physostigmine is a carbamate inhibitor of the enzyme acetylcholinesterase which was first isolated from Physostigma venenosum. Which of its functional group/s is/are essential for its activity?

    <p>All of the above (@)</p> Signup and view all the answers

    Which of the following statements is true regarding the structural features of muscarinic antagonists?

    <p>E) All of the above (@)</p> Signup and view all the answers

    What is the clinical indication of aryloxypropranolamines?

    <p>Hypertension (B)</p> Signup and view all the answers

    Which of the following statements describe the ideal antiepileptic drug?

    I. It should completely suppress seizures in doses that also cause sedation. II. It should be well tolerated, highly effective against various types of seizures and devoid of undesirable side effects on vital organs and functions III. Its onset of action should be rapid after parenteral injection for control of status epilepticus. IV. It should have a long duration of effect after oral administration for prevention of recurrent seizures.

    <p>II, III, and IV are correct (C)</p> Signup and view all the answers

    . Which of the following correctly describes the barbiturate 5-ethyl-5-phenylbarbituric acid?

    <p>D) A and B only (D)</p> Signup and view all the answers

    Which of the following statements correctly describe 2-ethyl-2-methylsuccinide?

    <p>A) It is widely accepted treatment of petit mal condition. (A)</p> Signup and view all the answers

    Which of the following statements correctly describe 5,5-diphenyl-2,4-imidazolidinedione?

    <p>A) B and C only (@)</p> Signup and view all the answers

    Which of the following statements correctly describe the structure-activity relationship of tricyclic psychotropic drugs?

    I. Optimal psychotropic activity is observed in ring systems that have a six-membered or seven-membered central ring. II. Dihenylalamine and Diphenylmethane derivatives that lack a central ring are devoid of psychotropic activity. III. Derivatives that contain a five-membered central ring lack psychotropic activity. IV. Rigidly planar tricyclic diphenylmethane derivatives such as anthracene are inactive.

    <p>I only is correct (A)</p> Signup and view all the answers

    Which of the following are pharmacologic responses elicited by phenothiazine?

    I. Antipsychotic effect II. Antiparkinsonian effect III. Anti-adrenergic, anticholinergic, antihistaminic and antiserotonin effects IV. Antiemetic effect

    <p>I,II,III,IV are correct (@)</p> Signup and view all the answers

    Which of the following drugs is/are a butyrophenone derivative?

    I. thioridazine II. Fluphenazine III. Droperidol IV. Haloperidol

    <p>III and IV are correct (D)</p> Signup and view all the answers

    A drug used in the treatment in myocardial insufficiency that is structurally similar to adenosine, a natural vasodilatory substance released by the myocardium during hypoxic episodes.

    <p>Dypirydamole (B)</p> Signup and view all the answers

    . An antiarrythmic drug composed of a quinoline ring and a bicyclic quinuclidine ring system connected by a hydroxymethylene bridge that is a member of a family of alkaloids found in cinchona

    <p>Quinidine (C)</p> Signup and view all the answers

    An antiarrythmic drug that is an ᾳ-methyl analog structurally related to monoethylglycinexylide, the active metabolite of xylocaine.

    <p>Tocainide (D)</p> Signup and view all the answers

    Which of the following statement is true regarding agonist at the H1 and H2 receptor antagonist of histamine?

    <p>A) A and B only (D)</p> Signup and view all the answers

    Which of the following statements correctly describes the ideal anesthetic agent?

    I. it should provide adequate muscular contraction II. It should produce rapid and uncomplicated induction and emergence III. It should have no effect on myocardium or respiration at anesthetic doses. IV. It should be non-flammable

    <p>III &amp; Iv only (@)</p> Signup and view all the answers

    Which f the following statement is true regarding anesthetics?

    I. Along with toxicity, increasing the chain length of ethers increases the anesthetic activity. II. Along with toxicity, increasing the chain length of ethers decreases the anesthetic activity. III. Introduction of unsaturation into an aliphatic ether increases potency and shortens induction and emergence IV. Introduction of unsaturation into an aliphatic ether decreases potency and shortens induction and emergence

    <p>I,III only (B)</p> Signup and view all the answers

    Which of the following statements is true regarding halogenated anesthetic agents?

    I. Addition of halogen atoms to ethers or hydrocarbons decreases flamability II. Addition of halogen atoms to ethers or hydrocarbons often increases anesthetic potency. III. Addition of halogen atoms to ethers or hydrocarbons decreases flamability IV. Addition of halogen atoms to ethers or hydrocarbons often decreases anesthetic potency.

    <p>I &amp; II only (A)</p> Signup and view all the answers

    Which of the following metabolic transformation of barbiturates can lead to loss of depressant activity?

    <p>All of the above (D)</p> Signup and view all the answers

    Which of the following acids has mycobacteriostatic activity?

    <p>Chaulmoogric acid (B)</p> Signup and view all the answers

    Which of the following alcohols has a local anesthetic property?

    <p>Benzyl alcohol (A)</p> Signup and view all the answers

    Which of the following amino ethers has antihistamine property?

    <p>Benzidioxanes (B)</p> Signup and view all the answers

    Which of the following halogenated compounds has hypnotic properties?

    <p>Chloral (C)</p> Signup and view all the answers

    Which of the following functional groups can decrease the absorption of cetirizine and clemastine through the blood brain barrier?

    <p>E) B and C (@)</p> Signup and view all the answers

    Which of the following functional groups can increase the absorption of cetirizine and clemastine through the blood brain barrier?

    <p>A) Aromatic hydrocarbon (A)</p> Signup and view all the answers

    If a truck driver asks you to recommend an antihistamine drug for his seasonal allergies, which of the two drugs will you recommend?

    <p>Cetirizine (B)</p> Signup and view all the answers

    A 35 year old woman comes to the pharmacy and asks you to recommend an antifungal cream rather than a spray or powder. You recommended terbinafine, an effective topical antifungal agent that is sold over the counter. What are the structural features/functional groups present in terbinafine that makes it an agent that can be used topically?

    <p>All of the above (@)</p> Signup and view all the answers

    Which among the following amino acids is likely to be present in the active site of the target enzyme of terbinafine and form an ionic interaction with the tertiary amine group?

    <p>Glutamic acid (D)</p> Signup and view all the answers

    Which among the following amino acids is likely to be present in the active site of the target enzyme of terbinafine and form an hydrophobic interaction with the aromatic hydrocarbons?

    <p>Phenylalanine (A)</p> Signup and view all the answers

    Wich of the following drugs is an ethylenediamine antihistamine?

    <p>Tripelennamine (A)</p> Signup and view all the answers

    Which of the following drugs in an example of tricyclic antihistamine?

    <p>Promethazine (C)</p> Signup and view all the answers

    Which of the following drugs is an example of an ethanolamine ether antihistamine?

    <p>Diphenhydramine (B)</p> Signup and view all the answers

    Which of the following drugs has a little or no sedative qualities?

    <p>Astemizole (D)</p> Signup and view all the answers

    According to this drug receptor theory, the number of drug receptor interactions per unit time determines the intensity of the biological response

    <p>Rate theory (A)</p> Signup and view all the answers

    This drug receptor theory suggest that the biological response is directly related to the number of receptors bound by an agonist.

    <p>Occupational theory (B)</p> Signup and view all the answers

    This drug receptor theory suggest that the drug approaches the receptor, a conformational change occurs in the receptor to allow effective binding.

    <p>. Induced fit theory (D)</p> Signup and view all the answers

    According to this theory, receptors are always in dynamic equilibrium between active and inactive states. Agonist function by shifting the equilibrium toward the activated state, whereas antagonist prevent the activated state.

    <p>Activation aggregation theory (C)</p> Signup and view all the answers

    This drug receptor theory suggest that two types of conformational changes exist and the rate of their existence determines the observed biological response.

    <p>Molecular pertubation theory (@)</p> Signup and view all the answers

    Which of the following statements correctly describes an agonist?

    <p>E) A and B (D)</p> Signup and view all the answers

    Which of the following statements correctly describes an antagonist?

    <p>C) They can bind to regions of the receptor that are not involved in binding the natural ligand (C)</p> Signup and view all the answers

    These are exogenous chemical messengers that act as antagonist, but also eliminate any resting acivity associated with a receptor.

    <p>. Inverse agonist (B)</p> Signup and view all the answers

    This condition may occur when an agonist is bound to its receptor for a long period of time.

    <p>Desensitization (B)</p> Signup and view all the answers

    This condition may occur when an antagonist is bound to a receptor for a long period of time. The cell synthesize more receptor to counter the antagonist effect.

    <p>Sensitization (A)</p> Signup and view all the answers

    This is a situation where increases doses of a drug over time to achieve same effect.

    <p>Tolerance (C)</p> Signup and view all the answers

    This is related to the body’s ability to adapt to the presence of a drug. On stopping the drug, withdrawal symptoms occur as a result of abnormal levels of target receptor.

    <p>Dependence (D)</p> Signup and view all the answers

    This is a measure of how strongly a drug binds to a receptor.

    <p>Affinity (B)</p> Signup and view all the answers

    This is determined by measuring the maximum possible effects resulting from receptor-ligand binding

    <p>Efficacy (C)</p> Signup and view all the answers

    This relates how effective a drug is in producing a cellular effect. It can be determined by measuring the concentration of drug required to produce 50% of the maximum possible effect.

    <p>Potency (A)</p> Signup and view all the answers

    These are molecules that act as substrates for a target enzyme, but which are converted into a highly reactive species as a result of the enzyme catalyzed reaction mechanism. The species formed then reacts with amino acid residues present in the active site to form covalents bonds, and act as irreversible inhibitors.

    <p>Suicide substrates (B)</p> Signup and view all the answers

    This type of inhibition binds to a different site other than the active site and can alter the shape of the enzyme such that the active site is no longer recognizable.

    <p>Allosteric inhibitors (C)</p> Signup and view all the answers

    These are enzyme inducers that are designed to mimic the transition state of an enzymecatalyze reaction mechanism. They bind more strongly than either the substrate or product.

    <p>Transition state analogue (A)</p> Signup and view all the answers

    The type of inhibitors that bind to the active site and compete with either substrate or cofactor.

    <p>Competitive inhibitor (D)</p> Signup and view all the answers

    Physostigmine inhibit which of the following enzyme?

    <p>Acetylcholinesterase (C)</p> Signup and view all the answers

    sildenafil, a drug for erectile dysfunction, inhibit which of the following enzyme?

    <p>3’,5’-cyclic GMP phosphodiesterase (D)</p> Signup and view all the answers

    . ethambutol, a drug for tuberculosis, inhibit which of the following enzyme?

    <p>Arabinosyl transferase (B)</p> Signup and view all the answers

    Which of the following drugs for diabetes inhibits the enzyme a-glucosidase?

    <p>Miglitol (B)</p> Signup and view all the answers

    Which of the following drugs for diabetes inhibits the enzyme a-amylase?

    <p>Acarbose (A)</p> Signup and view all the answers

    Which of the following drug (inhibitor)-enzyme inhibited pairs is incorrectly matched?

    <p>None of the choices (@)</p> Signup and view all the answers

    Which of the following drug (inhibitor)-enzyme inhibited pairs is incorrectly matched?

    <p>None of the choices (@)</p> Signup and view all the answers

    Which of the following drug (inhibitor)-enzyme inhibited pairs is correctly matched?

    <p>D) All of the above (D)</p> Signup and view all the answers

    Which of the following drugs (inhibitor) enzyme inhibited pairs is correctly matched?

    <p>All of the above (D)</p> Signup and view all the answers

    Which of the following phenolic drugs has an expectorant activity?

    <p>Guaiacol (B)</p> Signup and view all the answers

    Which of the following dyes is available as vaginal suppository for the treatment of yeast infection and has also been used orally as a anthelmintic for strongyloidiasis and oxyurias?

    <p>Methylrosaniline chloride (D)</p> Signup and view all the answers

    Which of the following dyes is a mixture of the chlorides of rosaniline and p-rosaniline? It is an ingredient of castellanis paint which is used topically in the treatment of fungal infection, such as ringworm and athletes foot?

    <p>Basic fuchsin (C)</p> Signup and view all the answers

    It is a non classical folate antagonist that is structurally similar to methotrexate. It inhibits the enzyme dihydrofolate reductase and has been approved for the treatment of pneumocystis carinii in patients with aids.

    <p>Trimetexrate (C)</p> Signup and view all the answers

    Which of the following anti-inflammatory analgesic is an arylacetic derivative that is comparable to aspirin in the treatment of rheumatoid arthritis, with a lower incidence of side effects? It has also been approved for used in primary dysmenorrhea.

    <p>Ibuprofen (C)</p> Signup and view all the answers

    Which of the following anti-inflammatory agents is an arylanthranilic acid derivative that has lower incidence of gastrointestinal bleeding than aspirin, and has been approved for use in the management of primary dysmenorrhea?

    <p>Mefenamic acid (B)</p> Signup and view all the answers

    Which of the following drugs is a derivative of aniline and has an analgesic and antipyretic properties? The FDA requires a warning label that read as follows: Warning: Do not give to children under 3 years of age or use for more than 10 days unless directed by a physician.

    <p>Acetaminophen (D)</p> Signup and view all the answers

    The following are synthetic estrogens except:

    <p>E) None of the choices (@)</p> Signup and view all the answers

    Which of the following estrogens is an estradiol metabolite originally obtained from the urine of horses especially pregnant mares?

    <p>Equilin sodium sulfate (A)</p> Signup and view all the answers

    Which of the following progestins is classified as a derivative of testosterone?

    <p>Megestrol acetate (A)</p> Signup and view all the answers

    Which of the following progestins are classified as derivative of testosterone?

    <p>A) Ethisterone (A)</p> Signup and view all the answers

    Which of the following prodrugs was designed to improve the membrane permeability of its active metabolite?

    <p>All of the above (@)</p> Signup and view all the answers

    Which of the following prodrugs was designed to prolong the drug activity of its active metabolite?

    <p>Azathioprine (B)</p> Signup and view all the answers

    Which of the following prodrugs was designed to lower water solubility of the active metabolite?

    <p>Chloramphenicol palmitate (C)</p> Signup and view all the answers

    Which of the following prodrugs was designed to mask the toxic side effects of its active metabolite?

    <p>Cyclophosphamide (A)</p> Signup and view all the answers

    Which of the following prodrugs was designed to increase the water solubility of the active metabolite?

    <p>Chloramphenicol succinate (D)</p> Signup and view all the answers

    Which of the following prodrug was designed to increase the chemical stability of the active metabolite?

    <p>Hetacillin (@)</p> Signup and view all the answers

    These are isomer that contain at least one assymetric, or chiral, carbon atom. Each asymmetric carbon atom can exist in one of two non-superimposable isomeric forms.

    <p>Optical isomer (A)</p> Signup and view all the answers

    This type of isomer occurs as a result of restricted rotation about a chemical bond, owing to double bond or rigid ring system in the molecule.

    <p>Geometric isomer (B)</p> Signup and view all the answers

    Also known as rotamers, these are non-superimposable orientation of a molecule which result from the rotation of atoms about single bonds.

    <p>Conformational isomer (C)</p> Signup and view all the answers

    Which of the following statements is true regarding ester-type local anesthetics?

    <p>B) They are generally short acting due to rapid hydrolysis in the plasma (B)</p> Signup and view all the answers

    Which of the following statements is true regarding amide-type local anesthetics?

    <p>A) They are generally long acting and are metabolized in the liver (A)</p> Signup and view all the answers

    Which of the following statements is true regarding the antipsychotic agents in the phenothiazine class?

    <p>D) A and B only (D)</p> Signup and view all the answers

    Which of the following pairs is correctly matched?

    <p>A) butyrophenone, haloperidol (A)</p> Signup and view all the answers

    Which of the following pairs of newer class of antipsychotic is correctly matched?

    <p>E) All of the above (@)</p> Signup and view all the answers

    Which of the following statements is true regarding tricyclic antidepressants?

    <p>B) Imipramine and clompramine are derivatives of dibenzazepine (D)</p> Signup and view all the answers

    Which of the following statements correctly describe the structure and mechanism of action of mao inhibitors?

    <p>D) A and B only (D)</p> Signup and view all the answers

    Certain metabolites retain the pharmacologic activity of their of their parent compounds to a greater or lesser degree. Which of the following drugs produce such metabolites?

    I. oxidation of the mercaptopurine II. Demethylation of morphine III. Dealkylation of iproniazid IV. Isomerization of retinoic acid

    <p>II only (D)</p> Signup and view all the answers

    Which of the following biotransformation produces a metabolite with an activity different from that of their parent compound?

    I. oxidation of the mercaptopurine II. Demethylation of morphine III. Dealkylation of iproniazid IV. Isomerization of retinoic acid

    <p>III, IV (C)</p> Signup and view all the answers

    Which of the following biotransformation produces a inactive metabolite

    I. oxidation of the mercaptopurine II. Demethylation of morphine III. Dealkylation of iproniazid IV. Isomerization of retinoic acid

    <p>I only (@)</p> Signup and view all the answers

    Which of the following statements is true regarding oxidation reaction?

    I. It is a most common phase 1 of biotransformation II. Oxidation reactions can occur in the liver III. The vast majority of oxidation is catalyze by a group or mixed function oxidases known as CYP450. IV. The increased polarity of the oxidized product (metabolites) enhances their water solubility and increases their tubular reabsorption to some extent, thus favoring their excretion in the urine

    <p>I and III Only (D)</p> Signup and view all the answers

    Which of the following statements is true regarding reduction reaction?

    I. It has same goal as oxidation reaction to create polar functional groups that can be easily excreted. II. Bacteria resident in the GI tract are also responsible for reductions of azo and nitro groups III. Chloramphenicol, sulfasalazine and acetohexamide can undergo reduction reaction IV. Cytochrome P450 enzymes is not involved in the reduction reaction

    <p>I, II, III (B)</p> Signup and view all the answers

    Which of the following drugs is metabolized by CYP1A?

    <p>All of the above (@)</p> Signup and view all the answers

    Which of the following drugs is metabolized by CYP4B?

    <p>prostaglandin (A)</p> Signup and view all the answers

    Which of the following statements is correct regarding Phase ll reactions?

    l.These are reactions in which the functional groups of the original drug(or metabolite)are masked by conjugation reaction ll.These reactions require both a high-energy molecules and an enzyme lll.High-energy molecules consist of a coenzyme bound to the endogenous substrate,the parent drug,or the drug’s phase l metabolite. lV.Most conjugates are highly polar and unable to cross cell membranes,making them almost almost always pharmacology inactive and of little or no toxicity.

    <p>l,ll,lll,lV (A)</p> Signup and view all the answers

    Flashcards

    Bond Polarity and Length

    As bond polarity increases, bond length decreases.

    Hybridization and Bond Length

    As s character increases, bond length decreases.

    Bond Strength

    Energy needed to break a bond in a diatomic molecule.

    Alkanes

    Saturated hydrocarbons that undergo combustion and halogenation.

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    Alkenes

    Unsaturated hydrocarbons known for addition reactions.

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    Aromatic Hydrocarbons

    Compounds based on benzene with unique bonding properties.

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    Water Soluble Alcohol

    Methanol is the most water soluble alcohol.

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    Oxidation of Alcohols

    Tertiary alcohols are ordinarily not oxidized.

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    General Formula for Ethers

    Compounds with the formula R-O-R, bonded to two carbons.

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    Aldehydes

    Compounds with the formula R-CHO, known for oxidation reactions.

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    Carboxylic Acid Functions

    Compounds with formula RCOOH, involved in salt formation and esterification.

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    Phase I Metabolic Reactions

    Reactions introducing new functional groups, making drugs more polar.

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    Phase II Metabolic Reactions

    Enzymatic reactions that increase polarity by adding groups.

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    Drug Absorption Rate Limiting Step

    Dissolution rate is the rate-limiting step for orally administered drugs.

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    Renal Excretion Processes

    Includes glomerular filtration, secretion, and tubular reabsorption.

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    Sulfonamides

    Antibacterial agents that inhibit microbial metabolism.

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    Penicillins

    Antibacterial agents inhibiting bacterial cell wall synthesis.

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    Polymyxins

    Antibacterial agents affecting bacterial plasma membrane permeability.

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    Trimethoprim

    Antibacterial agent that inhibits dihydrofolate reductase.

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    Salvarsan

    First synthetic antimicrobial drug used for syphilis and trypanosomiasis.

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    Drug Target Binding

    Drugs bind to targets via intermolecular forces.

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    Irreversible Inhibition

    Type of enzyme inhibition where the inhibitor forms a covalent bond.

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    Uncompetitive Inhibition

    Inhibitor binds to the enzyme-substrate complex.

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    Antagonists

    Bind to receptors but do not activate them.

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    Drug Enzyme Match

    Penicillins match transpeptidase for activity.

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    Stereochemical Isomers

    Biological activity can depend on the specific isomer form.

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    Hydrolysis of Esters

    Common decomposition pathway for drug molecules.

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    Lipid Solubility Effects

    Adding certain groups influences lipid solubility of drugs.

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