Pharmacology 2 Lec Finals PDF

 CUSHING SYNDROME PRESENTED BY: IMPERIAL  WHAT IS CUSHING'S SYNDROME? Cushing syndrome happens when the body has too much of the hormone cortisol for a long time. This can result from the body making too much cortisol, or from taking medicinces called...

 CUSHING SYNDROME PRESENTED BY: IMPERIAL  WHAT IS CUSHING'S SYNDROME? Cushing syndrome happens when the body has too much of the hormone cortisol for a long time. This can result from the body making too much cortisol, or from taking medicinces called glucocorticoids, which affect the body the same way as cortisol. - also called as Hypercortisolism  CAUSES RISK FACTORS Excessive production of cortisol (stress Age (25 to 50 yo) hormone) in thebody Gender (70% female, 30% male) Prolonged use of Glucocorticoids (e.g. People who take cortisol medication Prednisone, Dexamethasone). Pituitary adenoma Chronic Stress Conditions Nodular hyperplasia of the adrenal gland Obesity Uncontrolled type 2 diabetes Ectopic production of ATCH – caused by: Adrenal cortical adenoma; Lung, pancreas, thyroid and thymus tumors  MAIN SYMPTOMS Moon Face (round face) Fatty hump in neck Purple stretch marks (Purple (buffalo hump) striae) SYMPTOMS Hypertension Diabetes Red cheeks Easy bruising on the arms and legs General weakness and tiredness (fatigue) Osteoporosis Hypokalemia Weight gain Blurry vision and dizziness Weak muscles and thinner arms and legs Libido changes (sex drive) and erectile dysfunction Stunted growth in children Excessive hair growth  PHARMACOLOGIC THERAPY STEROID SYNTHESIS INHIBITORS MITOTANE METYRAPONE (Lysodren) (Metopirone) MOA Originally developed as an anti-cancer drug for adrenal MOA carcinoma, mitotane acts by destroying adrenal cortical cells an adrenal steroidogenesis inhibitor that selectively inhibits and inhibiting cortisol production. 11β-hydroxylase (CYP11B1) which is crucial for cortisol synthesis. SIDE EFFECTS SIDE EFFECTS Gastrointestinal upset Dizziness Lethargy Headache Dizziness Gastrointestinal disturbances Confusiol Adrenal crisis DRUG INTERACTIONS DRUG INTERACTIONS Anticoagulant drugs Medications metabolized by CYP450 enzymes Anticonvulsant drugs Warfarin  PHARMACOLOGIC THERAPY STERIOD SYNTHESIS INHIBITORS KETOCONAZOLE MIFEPRISTONE (Nizoral) (Mifeprex) MOA an antifungal imidazole derivative that is a nonselective MOA inhibitor of cholesterol side-chain cleavage, P450c17, C17, Mifepristone (RU-486) is a glucocorticoid receptor 20-lyase, 3β-hydroxysteroid dehydrogenase, and P450c11 antagonist that blocks the action of cortisol at its receptor enzymes required for steroid hormone synthesis. sites. This results in decreased glucocorticoid activity SIDE EFFECTS despite elevated serum cortisol levels. Nausea SIDE EFFECTS Vomiting Fatigue Abdominal pain Nausea Hepatotoxicity Vomiting Adrenal crisis Endometrial hyperplasia in women DRUG INTERACTIONS DRUG INTERACTIONS Medications metabolized by CYP450 enzymes CYP3A4 enzymes. Statins Benzodiazepines NON-PHARMACOLOGIC TREATMENT Trans sphenoidal adenomectomy or Hypophysectomy Transfrontal Carinotomy Bilateral Adrenalectomy Radiotherapy for Pituitary adenoma Dietary changes Stress Management Exercise THANK YOU KATEYKI !! ADDISON’S DISEASE PRESENTED BY: JAVIER, DASHA LEI M. Q3A INTRODUCTION Addison’s Disease is also called ADRENAL INSUFFICIENCY. A rare chronic condition in which adrenal glands don’t produce enough of the hormones cortisol and aldosterone Caused by an Autoimmune attack Addison’s disease can affect people 30 to 50 years old  TYPES 1.) Primary Adrenal 2.) Secondary Adrenal Insufficiency - Occurs Insufficiency - When the pituitary gland doesn’t make when the adrenal glands enough of the hormone ACTH are damaged. (Adrenocorticotropin). 3.) Tertiary Adrenal Insufficiency - When the hypothalamus doesn’t make enough corticotropin-releasing hormone. CAUSES RISK FACTORS AUTOIMMUNE RESPONSE TYPE 1 DIABETES TUBERCULOSIS HYPOPARATHYROOIDISIM HIV/AIDS HYPOPITUITARISM CANCER CELLS GRAVES’ DISEASE HEMORRHAGE IN ADRENAL VITILIGO GLANDS CHRONIC THYROIDITIS AMYLOIDOSIS DERMATITIS HERPETIFORMIS TESTICULAR FAILURE  SIGNS & SYMPTOMS Extreme fatigue Weight loss and loss of appetite Areas of darkened skin Low blood pressure, even fainting Salt craving Hypoglycemia Nausea, diarrhea, or vomiting People assigned female at birth with Addison’s disease may also have abnormal menstruation (periods), lose body hair, and have a decreased sexual drive.  PHARMACOLOGICAL TREATMENT CORTICOSTEROID MEDICATION MOA SIDE EFFECTS DRUG INTERACTIONS Weight gain, Hypertension, Synthetic form of cortisol, which Hydrocortisone Mood changes, Insomia, binds to glucocorticoid receptors (Cortef) Osteoporosis, Hyperglucemia, in various tissues. Skin thinning and bruising.. Binds to glucocorticoid receptors. Fluid retention and swelling, Prednisone (Rayos) It has a longer duration of action muscle weakness, gastric NSAIDs, Diuretics, compared to hydrocortisone. ulcers, increased appetite. Antidiabetic, Warfarin, Live Synthetic glucocorticoid that Vaccines mimics the action of cortisol. Insomia, Mood changes, Commonly used to reduce Methylprednisolone Hyperglycemia, Fluid inflammation and suppress the (Medrol) retention, Osteoporosis, immune system in various Hypertension, Weight gain. conditions (autoimmune disease & allergic reactions).  PHARMACOLOGICAL TREATMENT CORTICOSTEROID (MINERALCORTICOID) MEDICATION MOA SIDE EFFECTS DRUG INTERACTIONS Synthetic form of Hypertension mineralcorticoid. Binds to Edema ACE and ARBs Fludrocortisone mineralcorticoid receptors in the Hypokalemia Diurectics acetate (Florinef) kidneys leading to increased Headaches NSAIDs reabsorption of sodium and water. Heart Palipitations Increased excretion of potassium. GI upset NON-PHARMACOLOGICAL TREATMENT 1.) Stress Management 2.) Diet 3.) Self-Monitoring 4.) Regular Medical Check-Ups THANK YOU ! PHARMACOLOGY 2 CELL WALL INHIBITOR Amo, Rachelle Bacanto, Denirose Clamucha, Julianne Lanting, Francielle PENICILLIN 2 RINGS: BETA-LACTAM RING - Cyclic amide: the most important chemical nucleus of penicillin. THIAZOLIDONE RING - Sulfur-containing ring Contains Beta-Lactam Thiazolidine Ring; called 6-APA (6-Amino Penicillanic Acid) or the PENAM RING Naturally occurring and semi-synthetic can also be called antibiotics  3 TYPES OF PENICILLLIN NATURAL PENICILLINS These are not produced by humans, are present in our surroundings. To turn it into drugs, scientists extract (purify) only the penicillin that is present. SEMI-SYNTHETIC PENICILLINS To create more potent antibiotics, scientists modify the natural form of penicillin. These consist of extended- spectrum, amino, and penicillinase-resistant penicillin. COMBINATION MEDICATIONS To improve their effectiveness, penicillins are frequently mixed with other drugs to create a single medicine.  NATURAL PENICILLIN PENICILLIN G Pfizerpen AVAILABLE DOSAGE/FORMULATION PRECAUTIONS/WARNING/ADVERSE EFFECT Intravenous (IV) or Intramuscular (IM) - Allergic reaction (rash) 5 million units or 20 million units - Hyperkalemia or hypernatremia due to potassium or sodium content MECHANISM OF ACTION - Diarrhea, nausea, injection site reactions Penicillin G inhibits bacterial cell wall synthesis by binding to penicillin-binding DRUG/FOOD INTERACTIONS proteins, preventing peptidoglycan cross- Probenecid - Inhibits renal excretion linking. This weakens the cell wall, causing Aminoglycosides - Synergistic antibacterial bacterial lysis. effect when used together Oral Contraceptives - Reduce the MAIN INDICATIONS effectiveness of estrogen-containing Streptococcal infections, syphilis, contraceptives rheumatic fever prophylaxis Anticoagulants - Increase bleeding risk  NATURAL PENICILLIN PENICILLIN V Sumapen AVAILABLE DOSAGE/FORMULATION PRECAUTIONS/WARNING/ADVERSE EFFECT Oral tablets (250mg, 500mg) - Allergic reaction (rash) Oral Liquid Suspension (25 mg/5 mL, 250 - Hyperkalemia or hypernatremia due to mg/5 mL) potassium or sodium content MECHANISM OF ACTION - Diarrhea, nausea, injection site reactions Penicillin V inhibits bacterial cell wall synthesis by binding to penicillin-binding DRUG/FOOD INTERACTIONS proteins, preventing peptidoglycan cross- Same as Penicillin G except with linking. This weakens the cell wall, causing anticoagulants. bacterial lysis. Methotrexate - Potentially leading to toxicity MAIN INDICATIONS Mild to moderate infections such as strep throat, skin infections, otitis media, pharyngitis, and to prevent rheumatic fever.  SEMI-SYNTHETIC PENICILLIN: PENICILLINASE-RESISTANT NAFCILLIN OXCACILLIN DICLOXACILLIN Nallpen Bactocil Dynapen AVAILABLE DOSAGE/FORMULATION MAIN INDICATIONS Nafcillin: Injectable (IV/IM) Nafcillin: Used for Staphylococcal infections 500 mg, 1 g, 2 g vials like bacterial endocarditis, osteomyelitis, Oxacillin: Injectable (IV/IM) pneumonia, soft tissue infections, and sepsis. 250 mg, 500 mg, 1 g vials Oxacillin: Same as Nafcillin Dicloxacillin: Oral capsules or suspension Dicloxacillin: Used for skin and soft tissue 250 mg, 500 mg capsules; 125 mg/5 mL infections. suspension PRECAUTIONS/WARNING/ADVERSE EFFECT - Severe allergic reaction, including difficulty MECHANISM OF ACTION breathing and hypotension. Same as above. These penicillin are - Kidney inflammation in Nafcillin resistant to β-lactamase enzymes, making - Elevation in liver enzymes in Oxacillin. them effective against penicillinase- producing bacteria, Staphylococcus aureus. DRUG/FOOD INTERACTIONS Same as Penicillin G and V.  SEMI-SYNTHETIC PENICILLIN: AMINOPENICILLIN AMOXICILLIN AMPICILLIN Amoxil Omnipen AVAILABLE DOSAGE/FORMULATION MAIN INDICATIONS Amoxicillin: Oral Tablets (250 mg, 500 mg, Ampicillin and Amoxicillin are primarily used 875mg), Suspension (125 mg/5 mL, 250 to treat respiratory infections, urinary tract mg/5 mL), Injectable infections, ear infections, gastrointestinal Ampicillin: Oral Capsules (250 mg, 500 mg), infections, skin infections, and to prevent Suspension (125 mg/5 mL, 250 mg/5 mL), endocarditis in high-risk patients. Injectable (250 mg, 500 mg, 1 g, 2 g vials for PRECAUTIONS/WARNING/ADVERSE EFFECT IV/IM use) - Nausea - Rash MECHANISM OF ACTION - Diarrhea - Abdominal pain Same as above. These drugs bactericidal - Vomiting against Gram-positive and some Gram- DRUG/FOOD INTERACTIONS negative bacteria. Same as Penicillin G and V. Allopurinol - Increase the risk of skin rashes  SEMI-SYNTHETIC PENICILLIN: EXTENDED-SPECTRUM PIPERACILLIN AVAILABLE DOSAGE/FORMULATION PRECAUTIONS/WARNING/ADVERSE EFFECT Injectable (Intravenous) - Anaphylaxis and other severe allergic reactions - Electrolyte disturbances MECHANISM OF ACTION - Hepatotoxicity - Nephrotoxicity Same as above. DRUG/FOOD INTERACTIONS MAIN INDICATIONS Same as Penicillin G. Used to treat infections caused by susceptible bacteria, including intra- abdominal infections, respiratory tract infections, skin and soft tissue infections.  COMBINATION PENICILLIN AMOXICILLIN / CLAVULANIC ACID Augmentin AVAILABLE DOSAGE/FORMULATION MAIN INDICATIONS Oral Tablets: 250 mg/125 mg, 500 mg/125 Used to treat respiratory tract infections, skin mg, 875 mg/125 mg and soft tissue infections, urinary tract Oral Suspension: 125 mg/5 mL, 200 mg/5 infections, and middle ear infections. mL, 250 mg/5 mL, 400 mg/5 mL PRECAUTIONS/WARNING/ADVERSE EFFECT - Anaphylaxis and other severe allergic reactions MECHANISM OF ACTION - Electrolyte disturbances These drugs combine a β-lactam antibiotic - Hepatotoxicity with a β-lactamase inhibitor to prevent the - Nephrotoxicity breakdown of the antibiotic by β-lactamase DRUG/FOOD INTERACTIONS enzymes, allowing the antibiotic to inhibit - May reduce oral contraceptive effectiveness; bacterial cell wall synthesis and kill probenecid increases amoxicillin levels. susceptible bacteria. - Taking with food improves absorption and reduces gastrointestinal upset.  COMBINATION PENICILLIN AMPICILLIN / SULBACTAM Unasyn AVAILABLE DOSAGE/FORMULATION MAIN INDICATIONS Injectable Indicated for intra-abdominal infections, 1.5 g (ampicillin 1 g + sulbactam 0.5 g) gynecological infections, skin and soft tissue 3 g (ampicillin 2 g + sulbactam 1 g) infections, and sepsis. PRECAUTIONS/WARNING/ADVERSE EFFECT MECHANISM OF ACTION - Anaphylaxis and other severe allergic reactions These drugs combine a β-lactam antibiotic - Electrolyte disturbances with a β-lactamase inhibitor to prevent the - Hepatotoxicity breakdown of the antibiotic by β-lactamase - Nephrotoxicity enzymes, allowing the antibiotic to inhibit DRUG/FOOD INTERACTIONS bacterial cell wall synthesis and kill Probenecid prolongs blood levels of susceptible bacteria. ampicillin/sulbactam.  COMBINATION PENICILLIN PIPERACILLIN / TAZOBACTAM Zosyn AVAILABLE DOSAGE/FORMULATION MAIN INDICATIONS Injectable Used for severe intra-abdominal infections, 2.25 g (piperacillin 2 g + tazobactam 0.25 g), hospital-acquired pneumonia, complicated skin 3.375 g, 4.5 g and urinary tract infections, and sepsis. PRECAUTIONS/WARNING/ADVERSE EFFECT MECHANISM OF ACTION - Anaphylaxis and other severe allergic reactions These drugs combine a β-lactam antibiotic - Electrolyte disturbances with a β-lactamase inhibitor to prevent the - Hepatotoxicity breakdown of the antibiotic by β-lactamase - Nephrotoxicity enzymes, allowing the antibiotic to inhibit bacterial cell wall synthesis and kill DRUG/FOOD INTERACTIONS susceptible bacteria. ynergistic effect with aminoglycosides but avoid mixing in the same IV solution. CEPHALOSPORINS CEPHALOSPORINS are a large group of antibiotics derived from the mold Acremonium (previously called Cephalosporium). They bind to and block the activity of enzymes responsible for making peptidoglycan, an important component of the bacterial cell wall. Broad spectrum and more resistant to beta lactamase inactivation than penicillins. Structure: Consists of a six-membered dihydrothiazine ring fused to a beta lactam ring; called 7-ACA (Amino Cephalosporanic Acid) Mechanism of action: Act by interfering with bacterial cell wall synthesis. They bind to penicillin-binding proteins (PBPs), essential enzymes in the formation of the bacterial cell wall, inhibiting peptidoglycan crosslinking. 1ST GENERATION CEPHALOSPORINS More effective against gram-positive bacteria than on gram negative bacteria Excellent gram-positive and modest gram negative activity Alternatives for skin and soft-tissue infections, as well as for streptococcal pharyngitis. 1ST GENERATION CEPHALOSPORINS Route of Drug Name Brand Name(s) Spectrum of Activity Key Clinical Uses Administration Effective against Gram- positive cocci (Staphylococcus, Skin and soft tissue infections, Cephalexin Keflex, Keftab Oral Streptococcus); limited Gram- uncomplicated UTIs, respiratory negative coverage (E. coli, tract infections Klebsiella) Similar to cephalexin; good Surgical prophylaxis, skin activity against Gram-positive Cefazolin Ancef, Kefzol Intravenous (IV) infections, endocarditis cocci and some Gram-negative prevention in specific procedures bacilli Similar to cephalexin; Gram- Skin infections, respiratory Cefadroxil Duricef Oral positive cocci and limited infections, UTIs Gram-negative organisms SPECTRUM S - Staphylococcus/ Streptococcus P - Proteus EC - E. Coli K - Klebsiella 2ND GENERATION CEPHALOSPORINS Equally effective against gram-positive and gram- negative bacteria; if the causative agent is unknown it is good to suggest 2nd generation Have somewhat better activity against gram- negative organisms with some gram-positive action. Include agents with anti-anaerobe activity Used for treating URTI, LRTI, Sinusitis and otitis media 2ND GENERATION CEPHALOSPORINS Generic Brand Name Route of Administration Spectrum of Activity Key Clinical Uses Name - Active against gram-positive - Respiratory tract infections cocci (Streptococcus, Staphylococcus) (e.g., pneumonia, sinusitis, -Enhanced activity against gram-negative Cefuroxime Ceftin, Zinacef Oral, IV, IM organisms (e.g., H. bronchitis) influenzae, E. coli, Klebsiella, Proteus - Urinary tract infections (UTIs) mirabilis) - Skin and soft tissue infections - Similar to cefuroxime with less potent activity against gram-negative - Otitis media bacteria Cefaclor Ceclor Oral -Effective against H. influenzae, - Respiratory tract infections Moraxella catarrhalis, - Mild skin infections and Streptococcus pneumoniae - Surgical prophylaxis (especially - Broad spectrum with good activity against anaerobes (e.g., for abdominal surgeries) Cefoxitin Mefoxin IV Bacteroides fragilis) - Mixed aerobic/anaerobic -Moderate gram-positive and gram- infections (e.g., intra-abdominal or negative coverage pelvic infections) - Good activity against gram-positive cocci (Streptococcus - Respiratory tract infections pneumoniae, Staphylococcus aureus) Cefprozil Cefzil Oral -Moderate activity against gram-negative - Skin and soft tissue infections organisms (H. - Otitis media influenzae, Moraxella catarrhalis) SPECTRUM H - Haemophilus E - Enterobacter N - Neisseria S - Staphylococcus/ Streptococcus P - Proteus EC - E. Coli K - Klebsiella  3RD GENERATION CEPHALOSPORINS Cefotaxime and ceftizoxime (discontinued) offer the best gram-positive coverage out of all the third-generation agents; ceftazidime and cefoperazone (discontinued) are unique in that they provide antipseudomonal coverage. Ceftriaxone has a long half-life which allows for once daily dosing and may be used for the treatment of gonorrhea, pelvic inflammatory disease, and epididymo-orchitis. It is also an alternative to penicillins for suspected meningitis. All the third-generation cephalosporins except for cefoperazone (discontinued) penetrate cerebrospinal fluid. 3RD GENERATION CEPHALOSPORINS Generic Brand Name(s) ROA Spectrum of Activity Key Clinical Uses Name Broad spectrum: Effective against Gram-negative bacteria (e.g., E. coli, Klebsiella, H. Community-acquired pneumonia, Ceftriaxone Rocephin IV, IM influenzae) and some Gram-positive bacteria meningitis, gonorrhea, intra-abdominal (Streptococcus infections, and severe sepsis spp., S. pneumoniae) Similar to ceftriaxone; broad Bacterial meningitis, sepsis, Cefotaxime Claforan IV, IM spectrum, covering Gram-negative and some pneumonia, urinary tract infections (UTIs), and Gram-positive bacteria skin/soft tissue infections Nosocomial infections (e.g., Broad Gram-negative coverage, pneumonia), complicated UTIs, and infections Ceftazidime Fortaz, Tazicef IV, IM including Pseudomonas aeruginosa; caused by Pseudomonas less effective against Gram-positive bacteria aeruginosa Effective against Gram-negative bacteria (e.g., H. influenzae, Upper and lower respiratory tract Cefdinir Omnicef Oral M. catarrhalis, E. coli) and some Gram-positive infections (e.g., bronchitis, sinusitis, pneumonia) bacteria (S. pneumoniae)  Gram-negative bacteria (e.g., E. coli, H. UTIs, otitis media, pharyngitis, Cefixime Suprax Oral influenzae, Klebsiella, Proteus) uncomplicated gonorrhea, and and limited Gram-positive coverage bronchitis Gram-negative bacteria (e.g., E. coli, H. Acute otitis media, pharyngitis, Cefpodoxime Vantin Oral influenzae) and Gram-positive bacteria (S. sinusitis, community-acquired pneumoniae, Streptococcus pyogenes) pneumonia, and UTIs Broad spectrum: Effective against Gram-negative bacteria (E. coli, Intra-abdominal infections, Cefoperazone Cefobid IV, IM Pseudomonas aeruginosa, biliary tract infections, and Klebsiella) and Pseudomonas infections Gram-positive bacteria (Staphylococcus spp.) Mainly effective against Acute bacterial exacerbations Gram-negative bacteria (E. coli, of Ceftibuten Cedax Oral Klebsiella, Proteus) with limited Gram-positive chronic bronchitis, otitis coverage media, and uncomplicated UTIs SPECTRUM B - Borrelia P - Pseudomonas H - Haemophilus E - Enterobacter N - Neisseria S - Staphylococcus/ Streptococcus P - Proteus EC - E. Coli K - Klebsiella 4TH GENERATION CEPHALOSPORINS Equally effective against gram-positive and gramnegative bacteria but have extended spectrum against negative gram bacteria compared to the other generations Known as reserved agent Encompass the antimicrobial spectrum of all the third generation agents and have increased stability to hydrolysis by inducible chromosal-lactamases 4TH GENERATION CEPHALOSPORINS Drug Name Brand Name Route of Administration Spectrum of Activity Key Clinical Uses Broad-spectrum: Gram- Severe infections: pneumonia positive (e.g., MSSA, (including healthcare- streptococci), Gram- associated), febrile neutropenia, Cefepime Maxipime Intravenous (IV) negative (e.g., Pseudomonas urinary tract infections (UTIs), aeruginosa, Enterobacter intra-abdominal infections, skin spp.), some β-lactamase- and soft tissue infections. producing bacteria (Not FDA- Similar to cefepime: Severe nosocomial infections, approved in Effective against Gram- sepsis, and infections caused by the U.S.; Cefpirome Intravenous (IV) positive and Gram-negative drug-resistant bacteria in available in organisms, including some certain regions (e.g., Europe, other multidrug-resistant strains Asia). regions) SPECTRUM P - Pseudomonas E - Enterobacter N - Neisseria S - Staphylococcus/ Streptococcus 5TH GENERATION CEPHALOSPORINS It is active against methicillin-resistant Staphylococcus aureus (MRSA) and gram- positive bacteria. It also retains the activity of the later-generation cephalosporins and is effective against susceptible gram- negative bacteria. 5TH GENERATION CEPHALOSPORINS Route of Generic Name Brand Name Spectrum of Activity Key Clinical Uses Administration Broad-spectrum: Gram- Community-acquired positive (including bacterial pneumonia Ceftaroline Teflaro (US) Intravenous (IV) MRSA) and Gram- (CABP), complicated negative (E. coli, skin and soft tissue Klebsiella, Proteus spp.) infections (cSSTIs) Gram-positive (including MRSA, Hospital-acquired penicillin-resistant pneumonia (HAP), Ceftobiprole Zeftera (EU/CA) Intravenous (IV) Streptococcus complicated skin and pneumoniae) and Gram- soft tissue infections negative MONOBACTAM Monobactams are drugs with a monocyclic β- lactam ring. Their spectrum of activity is limited to aerobic Gram-negative organisms (including P aeruginosa). Unlike other β-lactam antibiotics, they have no activity against Gram- positive bacteria or anaerobes.  MONOBACTAM AZTREONAM Azactam / Cayston AVAILABLE DOSAGE/FORMULATION MAIN INDICATIONS Solution, inhalation Infections resistant to beta lactamses produced by gram 75mg (-) rods including Klebsiella, Pseudomonas & Serratia. Powder for injection Infections caused by aerobic, Gram-negative bacteria in 1g patients with immediate hypersensitivity to penicillins 2g MECHANISM OF ACTION PRECAUTIONS/WARNING/ADVERSE EFFECT Binds to penicillin-binding proteins; inhibits Precautions/Warnings: transpeptidation in bacterial cell walls. Use cautiously in those with penicillin/cephalosporin Prevents bacterial cell wall synthesis by allergies, renal impairment, or during pregnancy binding to and inhibiting cell wall (Category B). Prolonged use may cause superinfection. transpeptidases ADVERSE EFFECT: DRUG/FOOD INTERACTIONS Common: rash, fever, nausea, diarrhea, injection site pain. Probenecid: May increase aztreonam levels Serious: anaphylaxis, hepatotoxicity, renal toxicity, C. by decreasing renal excretion. difficile diarrhea. CARBAPENEMS The carbapenems are structurally related to other β-lactam anti biotics  CARBAPENEMS Imipenem + Cilastatin Primaxin IM, Primaxin IV AVAILABLE DOSAGE/FORMULATION MAIN INDICATIONS IV administration Wide coverage against gram (+) & gram (-) bacteria 1 gm/vial For serious infections such as pneumonia & sepsis MECHANISM OF ACTION DRUG/FOOD INTERACTIONS Prevents bacterial cell wall synthesis by binding to and inhibiting cell wall Drug Interactions: transpeptidases. May increase the risk of seizures with ganciclovir. Rapid bactericidal activity against Probenecid can raise plasma levels and half-life. susceptible bacteria May enhance the anticoagulant effect of warfarin. CILASTIN inhibits renal metabolism Reduces valproic acid levels, potentially impairing (hydrolysis) of imipenem by seizure control. DEHYDROPEPTIDASE. Lab Interference: Note: Can cause a positive direct Coombs' test. Administered together with an inhibitor of renal Interferes with urinary glucose tests using Clinitest®. dehydropeptidase, cilastatin, for clinical use.  CARBAPENEMS Imipenem + Cilastatin Primaxin IM, Primaxin IV PRECAUTIONS/WARNING/ADVERSE EFFECT CNS effects (seizures, confusion), blood disorders (eosinophilia, neutropenia), tachycardia, hearing loss, gastrointestinal issues (diarrhea, nausea), and injection site reactions. Rare effects include hepatic failure, dizziness, renal changes, rash, and hypotension. Serious reactions like anaphylaxis, C. difficile-associated diarrhea, and pseudomembranous colitis are also possible.  CARBAPENEMS Ertapenem Invanz AVAILABLE DOSAGE/FORMULATION MAIN INDICATIONS IV administration Wide coverage against gram (+) & gram (-) bacteria 1 g/vial For serious infections such as pneumonia & sepsis MECHANISM OF ACTION DRUG/FOOD INTERACTIONS Prevents bacterial cell wall synthesis by Reduces valproic acid levels, potentially impairing binding to and inhibiting cell wall seizure control. transpeptidases. Probenecid increases the concentration of Rapid bactericidal activity against doripenem. susceptible bacteria longer half-life allows for once-daily PRECAUTIONS/WARNING/ADVERSE EFFECT dosing, lacks activity versus Upset stomach, headache, nausea, vomiting, or Pseudomonas aeruginosa and diarrhea. Acinetobacter  CARBAPENEMS Doripenem Doribax AVAILABLE DOSAGE/FORMULATION DRUG/FOOD INTERACTIONS IV administration Probenecid increases the concentration of 500 mg MECHANISM OF ACTION doripenem. No significant food interactions noted. Similar activity to imipenem; stable to renal dehydropeptidase, lower incidence of seizures PRECAUTIONS/WARNING/ADVERSE EFFECT Precautions: Caution in patients with a history of MAIN INDICATIONS seizures, renal impairment, or hypersensitivity Complicated intra-abdominal infections reactions to beta-lactams. Complicated urinary tract infections Adverse Effects: Includes nausea, diarrhea, rash, Nosocomial pneumonia headache, and elevated liver enzymes. Serious side Skin and soft tissue infections effects include seizures, hypersensitivity reactions, Gram-negative infections (particularly in and superinfections. hospitalized patients)  CARBAPENEMS Meropenem Merrem IV AVAILABLE DOSAGE/FORMULATION MAIN INDICATIONS IV administration Complicated skin infections: Staph. aureus 1g/vial (methicillin-susceptible), Strep. pyogenes, Strep. 500 mg agalactiae, viridans strep, Entero. faecalis (non- VRE), Pseudomonas aeruginosa, E. coli, Proteus MECHANISM OF ACTION mirabilis, Bacteroides fragilis, Similar activity to imipenem; stable to renal Peptostreptococcus species. dehydropeptidase, lower incidence of Complicated appendicitis and peritonitis: seizures Viridans strep, E. coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Bacteroides fragilis, B. DRUG/FOOD INTERACTIONS thetaiotaomicron, Peptostreptococcus species. May lower valproic acid levels, increasing Bacterial meningitis: Strep. pneumoniae, H. seizure risk. Increases serum levels and half- influenzae (non-b-lactamase), Neisseria life with probenecid. May enhance warfarin's meningitidis. anticoagulant effects.  CARBAPENEMS Meropenem Merrem IV PRECAUTIONS/WARNING/ADVERSE EFFECT Contraindications: Hypersensitivity to meropenem or other carbapenems. History of severe allergic reactions to ß-lactam antibiotics. Precautions: CNS disorders, renal/hepatic impairment, pregnancy, and lactation. Use with caution in neonates and children. Adverse Reactions: Significant: CNS effects (seizures, delirium), severe skin reactions (AGEP, SJS, TEN, DRESS). Other: Thrombocytosis, GI issues (nausea, diarrhea), injection site pain, headache, rash. Potentially Fatal: Anaphylaxis, C. difficile-associated diarrhea. Pregnancy Category: B (IV/Parenteral). GLYCOPEPTIDE Glycopeptide antibiotics are a class of drugs of microbial origin, which work by inhibiting peptidoglycan synthesis — the antecedent of cell walls.  GLYCOPEPTIDE VANCOMYCIN Firvanq, Vancocin AVAILABLE DOSAGE/FORMULATION ADVERSE EFFECT Vials: 500 mg , 1 g, 5 g, 10 g irritating to tissue( phlebitis at the Oral tablets: 125-500mg injection site) IV infused: 500mg (30mins) Chills and fever 1000mg 60mins/ 12 hours Ototixicity- rare Nephrotoxicity MECHANISM OF ACTION “Red man syndrome” Inhibits cell wall synthesis by binding to the D- Ala-D-Ala terminus of nascent peptidoglycan. DRUG INTERACTIONS Nephrotoxic Agents INDICATIONS Muscle Relaxants Infections caused by Gram-positive bacteria Anesthetics ( sepsis, endocarditis, and meningitis) C alicile colitis (oral formulation)  GLYCOPEPTIDE TELAVANCIN Vibativ AVAILABLE DOSAGE/FORMULATION INDICATIONS Vials: 250 mg/vial , 750mg/vial Complicated skin and soft tissue infections hospital- acquired pneumonia MECHANISM OF ACTION PRECAUTIONS/WARNING/ADVERSE EFFECT Teratogenic ( avoid in pregnant women) 1. Inhibits cell wall synthesis by binding to Nephrotixicity the D-Ala-D-Ala terminus of nascent peptidoglycan. 2. It disrupts the bacterial cell membrane DRUG INTERACTIONS potential and increases membrane Abacavir permeability. Aceclofenac acemetacin Acetaminophen  GLYCOPEPTIDE TEICOPLANIN Targosid AVAILABLE DOSAGE/FORMULATION Intramuscular Oral PRECAUTIONS/ WARNING Intravenous Hypersensitivity or history of neutropenic MECHANISM OF ACTION reaction to vancomycin. Renal impairment Inhibits cell wall synthesis by binding to the Children D-Ala-D-Ala terminus of nascent Pregnancy and lactation peptidoglycan. INDICATIONS DRUG INTERACTIONS Community-acquired pneumonia aminoglycosides, colistin, amphotericin B, Complicated skin and soft tissue infections ciclosporin, cisplatin, furosemide, and Complicated urinary tract infections etacrynic acid. (Ototoxicity/ Nephrotoxicity) Hospital-acquired pneumonia  GLYCOPEPTIDE DALBAVANCIN ORITAVANCIN Both are semisynthetic lipoglycopeptide derived from teicoplanin. Same MOA w/ Vancomycin and Teicoplanin. Dosing: Oritavancin- 1200 mg, single dose Dalvabancin- 1000mg, Once weekly ORITAVANCIN Disruption of cell membrane permeability and inhibition of RNA synthesis. LIPOPEPTIDE A lipopeptide antibiotic is a type of antibiotic that exerts its antibacterial activity by binding to the peptidoglycan intermediate Lipid II, disrupting bacterial cell wall synthesis.  LIPOPEPTIDE DAPTOMYCIN Cubicin AVAILABLE DOSAGE/FORMULATION ADVERSE EFFECT IV powder for injection (350 mg; 500 mg) GI disturbances IV solution (1000 mg/100 mL-NaCl 0.9%; rash 350 mg/50 mL-NaCl 0.9%; 500 mg/50 mL-NaCl headache 0.9%; 700 mg/100 mL-NaCl 0.9%) rarely muscle discomfort/weakness MECHANISM OF ACTION Binds to cell membrane, causing depolarization and rapid cell death CONTRAINDICATION pediatric patients younger INDICATIONS than one year of age Infections caused by Gram-positive bacterla including sepsis and endocarditis. MRSA and vancomycin resistant skin and soft tissue infections. THANK YOU!  AMBATA, PAMAN, PAREDES, PHODACA PROTEIN SYNTHESIS INHIBITORS What is it? Protein Synthesis Inhibitors Protein synthesis inhibitors are a class of antibiotics that stop or slow the growth of new proteins by preventing bacterial ribosomes from synthesizing protein. They disrupt the process of protein synthesis by blocking the translation of mRNA into proteins within a cell.  Tetracyclines Available Drug & Food Medication MOA Indication Adverse Effects Dosage/Formulation Interactions Oral: 0.25–0.5 g four Tetracyclines times daily for adults; (Sumycin, 25–50 mg/kg/d for Dairy products Panmycin) children (8 years and Avoid in pregnancy (e.g., milk, cheese) older). Inhibit bacterial protein Used to treat and children