Questions and Answers
This medication is effective in treating ______ diseases, such as rheumatoid arthritis.
autoimmune
The side effects of the medication include ______ cystitis.
hemorrhagic
Polyclonal antibodies are sometimes used as a quick and potent ______ therapy to prevent the acute rejection reactions.
immunosuppressive
Antibodies can be prepared by ______ technology, which produces antigen-specific, monoclonal antibodies.
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Recombinant DNA technology can be used to replace part of the mouse gene sequence with ______ genetic material.
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Antilymphocyte globulins (ALG) and Antithymocyte globulins (ATG) are obtained from the ______ or serum of horses hyper-immunized with human lymphocytes.
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The half-life of the medication extends from ______ to 9 days.
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The medication is given i.m. or slowly infused ______.
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Ceftriazone disodium exists as ______ crystals.
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Cefpirome is used to treat susceptible ______ including urinary and respiratory tract infections.
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Ceftaroline fosamil is a prodrug that turns in vivo into ______ (the active metabolite).
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The resulted compound has the advantage that it is more ______-soluble.
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The oxime group in the C7 acyl moiety and a ______ ring attached to the central nucleus (C3 position) facilitate the increased activity against MRSA.
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Triamterene is an inhibitor of ______ channels.
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The parenteral formulation (600 mg powder for concentrate for solution for infusion) contains an equivalent amount of ceftoraline fosamil ______ solvate monohydrate.
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Sulfonamide group (—SO2NH2) is essential for the activity of ______ anhydrase inhibitors.
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The addition of amino group and a hydrogen to α and α1 position produces ______ compound.
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When the new acyl groups are derived from carboxylic acids, it shows good spectrum of antibacterial action for ______-positive bacteria.
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Carbonic anhydrase inhibitors must have an unsubstituted ______ group.
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[Blank] anhydrase inhibitors interfere with the reabsorption of HCO 3− in the proximal tubules.
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Intracellularly, ______ anhydrase converts H2O and CO2 to carbonic acid (H2CO3).
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The HCO3– is transported across the ______ membrane.
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Filtered bicarbonate is reabsorbed for every ______ secreted.
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Carbonic anhydrase inhibitors prevent the reabsorption of ______.
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Type I IFNs are induced by ______ infections.
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Fibroblasts and endothelial cells produce ______.
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IFN-γ is produced by ______ T lymphocytes.
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IFN-α is used to treat ______ B & C infections.
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IFN-β is used to treat ______ sclerosis.
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Diuretics increase the rate of ______ flow.
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Diuretics reduce extracellular fluid volume by decreasing total body ______ content.
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Diuretics inhibit the reabsorption of ______ ions.
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Exceptional osmotic diuretics like Mannitol don't cause ______ but produce diuresis
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The proximal tubule is ______ to water and solutes
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The thick ascending limb of the loop of Henle is permeable to ______ by Na+K+2Cl- Co transport
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The macula densa senses ______ conc. in filtrate and gives signal to J.G. Cells
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The J.G. Cells of afferent arterioles secrete ______ in response to low BP or low Na
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The early distal tubule is responsible for active transport of ______ by NaCl symport
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Aldosterone causes ______ absorption by Na+/H+/K+ exchange in the collecting tubule and collecting duct
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The proximal convoluted tubule is responsible for reabsorption of nearly 100% of ______ and amino acids
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Study Notes
Ceftriazone Disodium Properties and Uses
- Ceftriazone disodium exists as white crystals, soluble in water, and exhibits broad-spectrum activity against both gram-positive and gram-negative bacteria.
Cefpirome Properties and Uses
- Cefpirome is used to treat susceptible infections, including urinary and respiratory tract infections, skin infections, septicaemia, and infections in immuno-compromised patients.
- The intravenous dose for adults as sulphate is 1–2 g every 12 h over 3–5 min or infused over 20–30 min.
Ceftaroline Fosamil Properties and Uses
- Ceftaroline fosamil is a relatively recent approved cephalosporin from the fifth-generation.
- Ceftaroline is an oxyimino compound based on the structure of cefozopran (a fourth-generation representative).
- Ceftaroline fosamil is a prodrug that turns in vivo into ceftaroline (the active metabolite).
- The oxime group in the C7 acyl moiety and a 1,3-thiazole ring attached to the central nucleus (C3 position) facilitate the increased activity against MRSA.
SAR of Cephalosporins
- 7-Acylamino substitution:
- The addition of amino group and a hydrogen to α and α1 position produces a basic compound, which is protonated under acidic conditions of the stomach.
- The ammonium ion improves the stability of β-lactam of cephalosporins and makes them active orally.
- Activity against positive bacteria is increased, and gram-negative is decreased by acylation of the amino group.
- When the new acyl groups are derived from carboxylic acids, it shows good spectrum of antibacterial action for gram-positive bacteria.
Antibodies
- Antibodies are sometimes used as a quick and potent immunosuppressive therapy to prevent acute rejection reactions.
- Types of antibodies:
- Polyclonal antibodies:
- Antilymphocyte globulins (ALG)
- Antithymocyte globulins (ATG)
- Monoclonal antibodies:
- Rho (D) immunoglobulin
- Basiliximab
- Daclizumab
- Polyclonal antibodies:
Antibodies Preparation
-
- By immunization of either horses or rabbits with human lymphoid cells producing mixtures of polyclonal antibodies directed against a number of lymphocyte antigens (variable, less specific).
-
- Hybridoma technology:
- Produce antigen-specific, monoclonal antibody (homogenous, specific)
- Produced by fusing mouse antibody-producing cells with immortal, malignant plasma cells
- Hybrid cells are selected, cloned, and the selectivity of the clone can be determined
- Recombinant DNA technology can be used to replace part of the mouse gene sequence with human genetic material (less antigenicity - longer half-life)
- Antibodies from mouse contain Muro in their names
- Humanized antibodies contain ZU (humanized) or XI (chimeric) in their names
Antilymphocyte Globulins (ALG) & Antithymocyte Globulins (ATG)
- Polyclonal antibodies obtained from plasma or serum of horses hyper-immunized with human lymphocytes
- Bind to the surface of circulating T lymphocytes, which are phagocytosed in the liver and spleen, giving lymphopenia and impaired T-cell responses & cellular immunity
- Kinetics:
- Given i.m. or slowly infused intravenously
- Half-life extends from 3-9 days
- Uses:
- Combined with cyclosporine for bone marrow transplantation
- To treat acute allograft rejection
Interferons
- Families:
- Type I IFNs (IFN-α, β):
- Induced by viral infections
- Leukocyte produces IFN-α
- Fibroblasts & endothelial cells produce IFN-β
- Type II IFN (IFN-γ):
- Produced by Activated T lymphocytes
- Type I IFNs (IFN-α, β):
- Interferon types and uses:
- IFN-α:
- Hepatitis B & C infections
- Treatment of cancer (malignant melanoma)
- IFN-β:
- Multiple sclerosis
- IFN-γ:
- Treatment of chronic granulomatous diseases
- IFN-α:
Diuretics
- Diuretics are drugs that increase the rate of urine flow and also increase excretion of Na+ and an accompanying anion (negatively charged ion) like Cl–
- Diuretics reduce extracellular fluid volume (decrease in oedema) by decreasing total body NaCl content
- Compensatory mechanisms:
- Activation of the renin-angiotensin-aldosterone pathway
- The sympathetic nervous system
- Diuretics inhibit the reabsorption of Na+ ions, thereby reducing the quantity of water in body fluids
Carbonic Anhydrase Inhibitors
- Derived from sulphonamide antibacterials
- Sulfonamide group (—SO2NH2) is essential for its activity
- Inhibit carbonic anhydrase enzyme in the membrane and cytoplasm of the epithelial cells
- Primary site of action is proximal tubules
- Interfere with the reabsorption of HCO3–
Nephron Parts and Characters
- Proximal Tubule:
- Leaky - Freely permeable to water, solutes
- Active absorption of:
- Sodium Chloride
- Sodium Bicarbonate
- Glucose
- Amino Acids
- Organic Solutes
- Followed by passive absorption of water
- Loop of Henle:
- Descending limb: Permeable to water
- Thick ascending limb: Impermeable to water but permeable to sodium by Na+K+2Cl- Co transport
- About 25% of filtered sodium is absorbed here
- Macula Densa and Juxtaglomerular Apparatus:
- Contact between ascending limb with afferent arterioles - by specialized columnar epithelial cells Macula Densa
- Macula Densa sense NaCl conc. in filtrate
- Give signal to J.G. Cells present in afferent arterioles
- J.G. Cells of afferent arterioles secrete Renin
- RAAS in response to low BP, or Low Na:
- Renin-Angiotensinogen - Angiotensin I
- ACE-Angiotensin II
- Sympathetic, Aldosterone
- Vasoconstriction, Sodium and water retention
- Early Distal Tubule:
- Active transport of sodium by NaCl symport
- Calcium excretion is regulated (Parathomone and Calcitriol, increase absorption of calcium)
- Collecting Tubule and Collecting Duct:
- Aldosterone: On membrane receptor and cause sodium absorption by Na+/H+/K+ Exchange
- ADH: Collecting tubular epithelium permeable to water (Water enters through aquaporin-2)
Nephron Parts and Their Functions
- SEGMENT FUNCTION
- Glomerulus Formation of glomerular filtrate
- Proximal convoluted tubule Reabsorption of 65% of filtered Na+/K+/Ca2+, and Mg2+; 85% of NaHCO3, and nearly 100% of glucose and amino acids.
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Description
Learn about the properties and uses of Ceftriazone disodium and Cefpirome, including their solubility, antibacterial activity, and dosage instructions.
