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CR5 Pharmacology - Coggle Diagram

- - - - Nitrogen Mustards
        
        ADR
        
        metabolized product causes bleeding of bladder
        
        Haemorrhagic cystisis
        
        treated by Mesna
        
        ketchup
        
        Cyclophosphoamide
        
        prodrug
        
        Therapeutic uses
        
        lymphoma
        
        leukemia
        
        mayonaise
      - Platinum Compounds
        
        ADR
        
        Ototoxic
        
        a lot of vomiting (emunogenic)
        due to (+) 5-HT
        
        can be treated by ondansetron (5-HT antagonist)
        (kyle autocoid mnemonic oden food)
        
        Really nephrotoxic
        
        Therapeutic uses
        
        germ tumors and solid tumors
        
        Cisplatin
      - Nitrosourea
        
        Carmustine
        
        Therapeutic uses
        
        brain tumors bc its lipid soluble
      - causes cross-linking between strands (prevents double-stranded to be open) and formation of alkylating agents (triggers endonucleases) which prevents DNA synthesis
      - C for Cross linking
        
        they're the only drugs with a C
        
        ADR: Sterilityy
    - - prevents the synthesis of nucleotides and folates preventing DNA synthesis
      - Purine antagonists
        
        Mercaptopurine
        
        therapeutic uses
        
        Leukemia
        
        HGPT enzyme converts 6MP to compounds which inhibits the new formation of ribosyl-5-phosphate, as well as conversion to adenine and guanine nucleotides and where it induces strand breaks and base mispairing.
      - Pyrimidine antagaonists
        
        Fluorouracil
        
        messes with thymidylate synthetase which inhibits thymine synthesis
        
        Therapeutic uses
        
        Colorectal cancer
        
        ADR
        
        Skin plantar–palmar dermatitis
      - Folate antagonists
        
        Methotrexate
        
        inhibits DHFR enzyme and depleting intracellular FH4 which prevents synthesis of thymine (pyrimidine) and purines (AG).
        
        Therapeutic uses
        
        a lot of cancers
        
        immunosuppressant drugs
        
        ADR
        
        treated with leucovorin (folic acid)
      - Mercaptopurine & Methotrexate for anti-Metabolites
    - - Anthracyclines
        
        Doxorubicin
        
        inhibits topoisomerase II (DNA gyrase)
        
        function of DNA gyrase is to prevent supercoiling of DNA during replication, and it is an active process which requires ATP
        
        Therapeutic Uses
        
        breast cancer, lymphoma, solid tumors
        
        ADR
        
        Cardiotoxicity
        
        because it downregulates cardiac muscle proteins like troponin,myosin,actin leading to cell death
        
        -rubucin
        
        heart is red
      - Other
        
        Bleomycin
        
        During the G2 phase in interphase bleomycin cuts up the DNA into fragments
        
        Therapeutic uses
        
        germline cancers
        
        ADR
        
        Pulmonary fibrosis
        
        still unclear why
        
        BleoMYCIN for mucin for lung
      - They are called cytotoxic antibodies because they are extracted from streptomyces bacterium
      - both performed in G2 phase
        while topoisomerase activity is not restricted to G2, topoisomerase II's decatenation function is especially critical in this phase.
    - - Acts on microtubules and prevent mitosis from completing by freezing the metaphase stage
        
        Vinca Alkaloids
        
        vincristine,vinblastine
        
        ADR
        
        neurotoxicity
        
        blood related cancers: leukemia
        
        Taxanes
        
        -taxel
        
        paclitaxel
        
        solid tumors
        
        ADR
        
        neurotoxicity
        
        acts in metaphase and is neurotoxic
      - Other
        
        etoposide
        
        inhibits topoisomerase II
  - - - Glucocorticoids
        
        inhibition of lymphocyte proliferation helps in leukemia
        
        Predinolosone
      - GnRH analogues
        
        inhibition of gonadotropin release helps in germ cancers
        
        leuprolide
      - Estrogens
        
        Diethylstilbestrol
        
        Prostate tumors
      - Progesterone
        
        Medroxyprogesterone
        
        Endometrial Cancer
    - - Antiestrogens
        
        tamoxifen
        
        Premenopausal Breast Cancer
        
        T for Tits
      - Antiandrogens
        
        flutamide
        
        Prostate tumors
      - Aromatase Inhibitors
        
        anastrozole, letrozole
        
        Postmenopausal Breast Cancer
  - - - carcinogen lecture
  - - - binds and lyses lymphocytes
      - lymphoma
    - - prevents angiogenesis for cancer cells to receive blood supply
      - colorectal cancer
      - BEVArages and VEGetables
    - - breast cancer
      - binds to and inhibits the protein (HER2) which is overexpressed in breast cancer cells causing it to proliferate rapidly
      - T for Tits, GF for Girlfriend
  - - - +bleomycin in G2
- - - - prevent cell wall synthesis: x mycolic acid
      - oral only
  - - - not used in pregnancy
      - prevent proliferation
      - only taken on empty stomach
  - - - prevent cell wall synthesis: x arabinosyl transferase
      - orally and widely distributed
  - - - prevent things coming in and out of bacteria cell
      - dosage depends on weight and height of person
  - - - water soluble
      - messes with protein translation
- - - - drugs which can decrease preload (reduce blood volume) and afterload (vasodilation) are useful for heart failure
        
        ACEI and ARB are both arterial and venous dilators
      - delay of cardiac remodeling process
        
        makes the heart becomes fibrous and makes it harder to contract?
        
        patient has heart failure but can liver longer due to prolonged cardiac remodelling by drugs
- - - - How Cell Wall Inhibitors Work:
        -Beta lactams resembles the peptide
        -Beta-lactams causes the PBP to bind to it irreversibly causing cross-linking to fail
        -the cell wall to be weak and break if the bacteria tries to divide
        
        Beta-Lactam Resistant Pathogen
        some bacterias has beta-lactamases which breaks down the beta lactam preventing it to bind w the PBP
        Most common eg:
        -Staphylococcus aureus
        
        To combate this we have done multiple things:
        
        Beta-lactamase inhibitors,
        
        which will bind to the beta lactamase and prevent it from breaking down the beta lactams
        
        Methicillins
        
        has large side chain that will not fit into beta lactams
        
        Staph auerus combat against methicillins:
        created alternative binding sites that will prevent the beta lactams to binding onto the PBP enzyme
        
        we called these MRSA
        
        Treatment of MRSA:
    - - Cephalosporins
        
        General Rule:
        as you go up gram + treament decreases
        as you go up gram - treament increases
        Balance: if they can treat a lot of positive they can't treat a lot of negative
        fourth generation has speciality towards Psuedomonas aeurgenosa
        Fifth generation can treat MRSA and gram - bacteria
        
        Types
        
        Generation 1
        
        Cefazolin
        
        Person playing a violin in a decapitated room
        
        The only difference between gen 1 and gen 5 is that gen 5 can treat MRSA and gen 1 can't.
        other than that these two have the same characteristics
        
        Generation 2
        
        Ceferoxime
        
        person wearing a furry coat in a decapitated room
        
        Used for uncomplicated community acquired infections: RTI, UTI, skin infections
        
        Generation 5
        
        Ceftaroline fosamil
        
        person smoking taro in a line
        
        used for mild-moderate infections (pneumonia, soft tissue and skin infection) that has risk of MRSA
        
        does not cross BBB
        
        all types cannot treat enterococci infection like endocarditis, whereas penicillins can
        
        Generation 3
        
        Cefotaxime
        
        mechanic fixing a taxi
        
        Can cross blood-brain barrier
        
        Ceftazidime
        
        can treat P.aerugenosa
        
        if you flip the dime over you see the face of mona lisa
        
        the mechanic was paid with a giant dime
        
        room fill w books to rmb BBB
        
        Generation 4
        
        Most used to treat nosocomial infection (hospital acquired infection) because of their high resistance to beta-lactamases
        
        Cefepeme
        
        primate painting the mona lisa in a hospital bed
        
        ADR
        
        -can increase toxicity of alcohol if taken w alcohol
        -should not be taken with penicillins
        -can cause superinfection: pseudomembranous colitis
        
        Mneumonic
      - Penicillins
        
        Categorized by their spectrum (narrow,broad)
        
        penicillins aren't metabolized at all so its mostly excreted by kidney, and would need dose adjustments in dialysis
        
        Types
        
        Natural Penicillins
        
        Penicillin G (Benzylpenicillin)
        
        Most broad range hence can treat more systematic diseases except staph. aerus
        
        Extended Penicillins or Aminopenicillins
        
        Safe for pregnancy
        
        Amoxicillin
        
        mocking bird singing lullaby to a baby
        
        Broad range for non-complicated community aquired infections (UTI,RTI,meningitis)
        
        Anti-pseudomonal Penicillins
        
        piperacillin
        
        mona lisa eating pepper
        
        gram -, speciality: P.aeruginosa
        
        find out more on how to know if its an P.aeruginosa infection
        
        Anti-staphylococcal Penicillins
        
        cloxacillin, methicillin
        
        staphylococcal infection except MRSA
        
        has large side-chain making it resistant to beta-lactamase
        
        ADR
        
        Allergic reaction possibility is quite high
        
        will develop rash
        
        cross-activity with other beta-lactems, so if youre allergic to penicillin you might be allergic to other beta-lactems bc they are similar
        
        Superinfection: pseudomembranous colitis by c. difficil
      - Inhibitors of Beta-lactams
        
        can be used with penicillins to be more resistant towards beta-lactamase
        
        Examples:
        
        Clavulanic acid
        
        Sulbactam
        
        Tazobactam
        
        however doesn't work against: enterobacter,acinetobacter, and pseudomonas
      - Carbapenems
        
        Highly resistant to beta-lactams
        
        broad range and can work against p.aeruginosa and acinerbacter
        
        only given parentally
        
        ADR: more severe, hence why its given as second line choice of drugs for severe community acquired or hospital acquired infections
        
        Types
        
        Imipenem
        
        have to be given with cilastatin to prevent renal toxicity
        
        carb rich penne pasta
      - Monobactems
      - Glycopeptides
        
        vancomycin
        
        directly binds to the tetrapeptide chains hence does not have effect on PBP
        
        does not work on gram - bc it cannot breach their outermembrane barrier
- - - - bc SABA are rapid onset that means it is used for acute attacks
    - - Tiotropium
        
        binds mostly M3 (hence doesn't give cardiac tachycardia effect)
      - Ipratropium
        
        binds to both M2 and M3 hence can give tachycardia ADR
        
        should be given for ppl w cardiovascular problems and old age bc ppl w old age tend to have harder time beating the heart fast enough.
      - slow onset of action
  - - - does not relieve symptoms of acute asthma attacks
    - - ADR: "L" for liver toxicity