80 pharmacology things you should know.pdf

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    80 pharmacology things you should know

    Anthony Christanto

    1. There are many ways to transmit a drug to patient, and it mainly divided to two subgroups:enteral (which is means to digestive tract) and parenteral. Enteral includes oral,

    sublingual, and rectal, while parenteral includes intravenous, intramuscular, and

    subcutaneous. Others include inhalants, intranasal, intratecal, intraventricular, topical,

    and transdermal.

    2. Gram negative bacteria is more resistant to antibiotics than Gram positives. This isbecause antibiotics often work through the production of peptidoglycan, and Gram

    negatives walls are lack of peptidoglycan.

    3. Antibiotics purpose is mainly to treat the medically-important microorganisms. Theseincludes Gram-negatives coccus and bacillus, Gram-positives coccus and bacillus, Gram-

    negatives enteric bacillus, Spirochaeta, Mycoplasmas, Chlamydia, and other several

    microorganisms include Rickettsia and Amoebas. These determine the spectrum of an

    antibiotic.

    4. There are several ways of bacteria forming a resistance. There are: DNA spontaneousmutation, Target modification (MRSA), Efflux pump system (Tetracycline, Primaquine),

    and inactivation by enzyme (-lactamases).

    5. Irrational usage of antibiotics, include broad-spectrum or combinations, can cause aninfection caused by a resistant bacteria or fungi. This involves changes in normal floras in

    the human body, and being called as super infection.

    6. Penicillin is effective to gram-positives as they synthesize peptidoglycan in their wall.7. Penicillin is originally a narrow-spectrum. By attach various side chains, Penicillin gains

    broader spectrum and better absorption ability. For example, Adding amino makes

    penicillin an aminopen (aminopenicillin) which is often called extended-spectrum penicillin

    because of its broad spectrum against the Gram-negatives. Amoxicillin, one of the

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    aminopens, is widely used as prophylactic for oral surgery patients who suffer a heart valve

    disorders.

    8. Amoxicillin, one of the most frequently used antibiotics of the world recently, is often soldin the combination with clavulanate acidto prevent destruction by -lactamases.

    9. Penicillins most unwanted side effects include hypersensitivity (angioedema andanaphylactic shock), nephritis, and diarrhea.

    10.Penicillin is originally effective for Staphylococcus. PBP (Protein binding-penicillin)modification causes lower affinity towards penicillin and finally causes what we call MRSA

    (Methicillin-Resistant Staphylococcus Aureus).

    11.Penicillin causes no teratogenic effect, even though it can pass through the syncitio-throphoblast (the placenta barrier).

    12.Penicillin can pass through the blood brain barrier and bones only in the state ofinflammation. In normal state, this cannot happen.

    13.Cephalosporin 1st gen is effective for PEcK: Proteus mirabilis, Escherichia coli, and Klebsiellapneumoniae. 2

    ndgen is effective for HENPEcK: Add Haemophilus influenzae, Enterobacter

    aerogenes and Neisseria. 3rd

    gen is effective for above bacteria, in addition to Pseudomonas

    aeruginosa.

    14.All cephalosporin except Cefadroxil, Cephalexin, (1

    st

    gen) Cefaklor, Cefuroxim (2

    nd

    gen) andCefixim (3

    rdgen) must be given IV.

    15.Ceftriaxone may be given to patient with renal insufficiencies, as it is excreted throughfeces.

    16.Vancomycin is a glicopeptide in the same mechanism as penicillin, and is used to treatMRSA. However, the usage of this antibiotic is highly controlled to prevent resistance.

    17.Carbapenem, the newest weapon in the avalanche of antibiotics, is one of -lactams. It isused to treat MRSA and VRE (Vancomycin Resistant Enterococcus). It is also effective

    towards Pseudomonas aeruginosa.

    18.Aztreonam, the monobactam, is a narrow-spectrum -lactam. It is used for patient withallergy towards penicillin and cephalosporin.

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    19.There is a group called -lactamase inhibitorwhich anti-bacterial activity is not significant,but they inactive -lactamase. They include Clavulanate acid, Sulbactam, and Tazobactam.

    20.All sulfonamides used in clinic are synthetic PABA analogues.21.Pirimetamine, one of Sulfonamides, is used to treat Toxoplasmosis.22.Silver sulfadiazine is used to treat sepsis shock caused by major burn, topically.23.Older sulfonamides are likely to cause crystaluria if consumed without enough water

    consumption. They are indeed nephrotoxic.

    24.Sulfonamides must not be given into pregnant women as it can cause kernicterus. It islikely that sulfa replace bilirubin from its binding with serum albumin (in other words,

    increase the indirect bilirubin). With the same reason, neonates within 2 months of their

    early life are not permitted to consume sulfonamide.

    25.Sulfonamides side effect including the most severe form of hypersensitivity, the Stevens-Johnson syndrome.

    26.Trimethoprim is anti-folic just like sulfonamide, but it is often combined with sulfame-toxazole become what we know as cotrimoxazole.

    27.Trimethoprim inhibits the enzyme dihidrofolic reductase, while sulfonamide inhibitsDihydropteroic synthase.

    28.Sulfonamides, includes cotrimoxazole, increase the activity ofanti-coagulant. In conclusion,its usage must be carefully monitored upon patients who used anti-coagulant (Patients who

    have heart disordersare likely to used anti-coagulant).

    29.Tetracycline, Aminoglycoside, Macrolide, Chloramphenicoland Clindamycin are antibioticgroups which inhibit synthesize of bacterias protein.

    30.Tetracycline cannot be given with milk or antacids, except for doxycycline.31.Tetracycline can causepigmentation and growth disorderin bones and teeth, pass through

    the placenta barrier and cause same effects to the fetus.

    32.For the reasons above, Tetracycline do not be given to pregnant and lactating women andneonates, as it can also cause increasing intracranial pressure and cause cranial falsiforms.

    33.Doxycycline is the only tetracycline used to treat nephritis as it excreted through feces.Other tetracycline not to be given to patients with nephritis.

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    34.Tigecycline can be used to treat MRSA.35.Tetracycline is the drug of choice for cholera.36.Tetracyclines side effects include azotemia,peptic ulcer, and bone and teeth pigmentation

    and hypoplasia.

    37.Aminoglycoside is working in synergies with -lactams as it increases the diffusion ofaminoglycoside inside the bacteria.

    38.All aminoglycoside except neomycin should be given parenteral.39.Neomycin is used to sterilize the gut pre-surgery.40.Neomycin has the most nephrotoxic effect.41.Framicetine is a topical-used aminoglycoside for skin infections and burns.42.Elders should not consume aminoglycoside as they are vulnerable to nephrotoxic and

    ototoxic. Neonates are also vulnerable, so precaution for pregnant women is essential.

    43.The most feared side effect ofaminoglycoside is super infection by Pseudomonas.44.Erythromycin has the same spectrum as penicillin; therefore, it is used to treat penicillin-

    allergy patients.

    45.Erythromycin should not be given to patients with liver failure , as the drug accumulated inliver.

    46.Erythromycin and Clarithromycin is the only drugs that inhibit terfenadines, an anti-histamine, metabolism and can cause heart arrhythmia (torsade de pointe).

    47.Chloramphenicolis rarely usedbecause of its heavy side effects. It should not be given toneonates, for example, because it can cause Gray syndrome, a fatal cyanosis occurs in

    neonates. It only be considered given in a life-threatening state.

    48.Each protein synthase inhibitor antibiotics had their own way to inhibits protein synthaseprocess. Tetracycline inhibits 30S ribosome protein to script tRNA,Aminoglycoside causes

    30S ribosome to wrongly decipher genetic codes, Macrolidebinds the 50S ribosome and

    inhibits translocation, and Chloramphenicolinhibitspeptidyl transferase in 50S ribosome.

    Clindamycin has the same mechanism as macrolides.

    49.Quinolone is an antibiotic made from nalidixate acid, a urogenital tract antiseptic.50.Quinolone inhibits topoisomerase II enzymeof the bacteria so that its DNA cant replicate.

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    51.Quinolone are not allowed to treatpneumococcus and enterococcus infections.52.Ciprofloxacin is the most potent fluoroquinolone. It is often used as substitute for

    aminoglycoside and used to treat MRSA.

    53.Fluoroquinolone is not allowed to be consumed by pregnant and lactating women andneonates less than 8 years, as it causes articular cartilage erosion.

    54.Fluoroquinolones most unwanted side effects are the disorders of the CNS.55.Quinolone in the form ofnalidixate acidis effective for benign cystitis. For malign cystitis

    and other urogenital tract infections like prostatitis, fluoroquinolone is proven to work

    well.

    56.The antiviral drugs are divided into 4 subgroups, which are anti-respirational viralinfection, anti-herpes and CMV, anti-HIV, and interferon (anti-hepatitis).

    57.Amantadine and Rimantadine are anti-respirational viral infections especially for InfluenzaA. They inhibit the uncoating of the virus and are most effective when given 24-48 hours

    within the beginning of the symptoms.

    58.Amantadine and Rimantadine is embryotoxicand teratogenic. Their usages in pregnant andlactating women are given special precaution.

    59.Ribavirin, the other anti-viral for respirational infections, is effective for RSV(RespirationalSyncytial Virus) and Influenza. It inhibits synthesize of viral mRNA. It is indicated forchildren and babies. It can also treat hepatitis if combined with interferon.

    60.Ribavirin is also contra-indicated for lactating and pregnant women as it causesteratogenic effect.

    61.All anti-herpes and CMV are anti-metabolites and analogue of purine and pyrimidine.62.Anti-herpes and CMV are effective only for acute phase of the infection, and not in latent

    period of the virus.

    63.Acycloviris the most used anti-herpes because of its effectiveness through herpes virus 1,

    2, varicella-zoster virus, and Epstein-Barr virus. However, CMVis resistantto acyclovir.

    64.Acyclovir needs to be activated through one phosphate atom. It is effective to genitalherpes, and it inhibits viral DNA polymerase.

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    65.Gancicloviris derivate of acyclovir used to treat CMV. It is embryotoxic, carcinogenicandteratogenic.

    66.Famcicloviris derivate of acyclovir used to treat acute herpes zoster.67.Anti-hepatitis virus includes interferon, entecavir, ribavirin, and lamivudine. Except

    interferon, they are used to treat Hepatitis B.

    68.Interferon is not only an anti-viral, but also an anti-proliferative and immunosuppressant.69.Interferon is the most interferon used in clinic. It is used to treat Hepatitis B, C, and

    Kaposis sarcoma, a tumor caused by herpes virus 8.

    70.All anti-viral described above are anti-DNA viral, while anti RNA viralincludes the anti-HIV,and mainly the Transcriptase inhibitor: Nucleoside and nucleotide Reverse Transcriptase

    Inhibitors (NRTI), Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI), and Protease

    Inhibitors (PI).

    71.All anti-malaria is named after each stadium in which the drug works. There are bloodskizontosid (Chloroquine, Quinine, Mefloquine, Anti-folic, and halofantrin), Tissue

    skizontosid (proguanil, pyrimethamine), Gametosid (Kina and Chloroquine for P.vivax,

    ovale, and malariae, and primaquine for P.falciparum) and Sporontosid(Primaquine and

    Chloroguanide).

    72.Of all above anti-malarias, some are forbidden for lactating and pregnant women:Primaquine,Anti-folic, Halofantrin, Doxycycline, andArtemisinin.

    73.Chloroquine is also being used to treat Systemic Lupus Erythematossus. Kina can causeblack water fever.

    74.Atovaquon is an anti-malaria and anti-toxoplasmosis.75.Some of anti-toxoplasmosis includes Pyrimethamine, Sulfadiazine, Cotrimoxazole,

    Clindamycin, Spiramycin andAtovaquon.

    76.There are several circumstance in which anti-toxoplasmosis is used during pregnancy.

    Spiramycin is used when the mother is positively infected but the fetus is negatively

    infected, while spyramicin will reduce the riskof the baby being infected without having

    any risk. Pyrimethamine and Sulfadiazine is high-risk, but it is given to prevent further

    congenital damage while the baby ispositivelyinfected by toxoplasma.

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    77.Some anti-philariasis is diethyl carbamazine (the drug of choice), ivermectin, and Suramin.78.Ivermectin is not allowedfor pregnant women and infants.79.As an immunosuppressant, cyclosporine is safe for pregnant women. Ciprofloxacin is not

    tobe given for pregnant women unless an emergency state.

    80. The writer of this note reallywants you to get good score for tomorrows test.