Farmakologi

The exercise was created 2023-01-07 by YeetMcYeet. Question count: 120.

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  • OTC receptfritt
  • causal therapy attacks the cause of the disease (infection)
  • symptomic therapy relieves or reverses the cause of the disease (anti-inflammatory)
  • substitution therapy replaces endogenous substance (insulin)
  • prophylactic therapy prevents diseases (vaccin)
  • pharmacodynamics what the drug does to the body, what the body does to the drug
  • pharmacokinetics what the body does to the drug, what the drug does to the body
  • hormones are transported long way via blood stream to then interact with membrane bound receptors on target cells
  • Electrical impulses in nerve cells will release neurotransmitters close to the target cell
  • agonist bind to receptor and induce cell respons, bind to receptor and prevent induction of respons from endogenous ligand
  • antagonist bind to receptor and prevent induction of respons from endogenous ligand, bind to receptor and induce cell respons
  • mycket kan binda till plasman - men plasma räknas inte som en receptor sant, falskt, det beror på
  • ligand gated ion channels alter ion permeability -> alter membrane potential
  • ionotropic receptor ligand-gated ion channel
  • metabotropic G-protein coupled receptors
  • 4 stora receptor families ligand gated ion channel, G-protein, kinase linked, nuclear receptors
  • G-protein coupled receptor ligand ändrar konformation -> förändrad affinitet (receptor & G-prot)
  • nuclear och kinase-linked receptors timmar, sekunder, millisekunder
  • G-protein coupled receptors hastighet sekunder, millisekunder, timmar
  • ligand-gated ion channels hastighet millisekunder, sekunder, timmar
  • COX/cyklooxygenas enzym skapar prostaglandiner som deltar i inflammation
  • Efficacy Magnitude of agonist-induced response
  • full agonist inducerar maximal respons, sub-maximal respons
  • partial agonist sub-maximal respons, inducerar maximal respons
  • Potency effect related to agonist concentration
  • Drug A och B når Emax vid olika konc, A är mest potent eftersom den har lägst EC50
  • EC50 effective concentration, (konc som ger 50% av max respons)
  • ED50, effective dose typ EC50 in vivo. 50% av patienter når önskad effekt
  • spare receptors fulla agonister behöver inte alla receptorer. Blir några kvar
  • Receptor desensitization, desensitization decreased responsiveness after repeated exposure to agonist
  • vid desensitization kan en full agonist och kvarvarande receptorer generera max effekt
  • Desensitization, Tolerance, Resistance Decreased response to drug treatment
  • IC50 konc av antagonist som minskar agonist respons med 50%
  • Competitive receptor antagonist antagonist bind reversible to the same site as the agonist
  • Noncompetitive receptor antagonism antagonist bind irreversible to the same site as the agonist or to an allosteric site
  • Systemic effect drug reach the systemic circulation (whole body)
  • Local effect effect at the application site
  • drugs passage across cell membranes beror på deras Chemical properties tex, om de är fett-eller vattenlösliga
  • anledningar till Desensitization Internalization of receptors, Decreased synthesis, Changes in the receptor protein, Changes of transducer proteins, Changes in second messenger system
  • diffusion absorption pathway for most drugs
  • Bioavailability the fraction of the given dose that reaches systemic circulation in active form (unchanged)
  • drugs som ges orally kommer till levern först, där sker first passage metabolism vilket bryter ner den och distribuerar den
  • drugs administered IV enter directly into the systemic circulation and have direct access to the rest of the body
  • både free och bound drugs finns i cirkulationen. Men bara free drugs kan diffuse och binda till receptorer
  • Volume of distribution, vd amount of drug in the body / plasma concentration
  • Active metabolites, Toxic metabolites, Prodrugs undantag för att metabolism inte gör drogen inaktiv
  • Prodrugs inactive compound is metabolized to the active form
  • Toxic metabolites drug skapar något giftigt
  • Active metabolites (ett fåtal bara) drugs blir mer aktiva efter metabolismen
  • First-order kinetics The amount of drug metabolized per unit time is proportional to the plasma konc of the drug.
  • First-order kinetics T1/2 Fixed half life time
  • Zero-order kinetics Metabolizing capacity is saturated, a constant amount of drug is metabolized per unit time
  • therapeutic window var drug ger bra effekt, inte side effekt eller ingen effekt (typ)
  • steady state Equilibrium is reached after repeated dosing of drug. Taken amount=amount eliminated
  • minskad elimination, minskad absorption, ökad metabolism minskad kidney function resulterar i (tänk ADME)
  • minskad distribution, ökad elimination, ökad absorption, minskad metabolism minskad circulation resulterar i (tänk AMDE)
  • typeA, typeB vanlig side effekt - predictable and dose dependent
  • pro drug drug som måste genomgå metabolism innan det blir aktivit
  • direkt, inte-alls, indirekt GPIIb/IIIa-antagonister påverkar platelet aggregation __
  • indirekt, direkt, inte-alls dipyridamole påverkar platelet aggregation __
  • indirekt, direkt, intealls P2Y12-antagonister påverkar platelet aggregation __
  • X, V, VIII, XI i koaguleringsprocessen aktiveras flera olika koaguleringsfafktorer av trombin. Vilken aktiveras inte av trombin?
  • det finns redan färdiga koagulerings faktorer, det tar tid innan det sprids i kroppen, det påverkar så många faktorer så det tar tid varför tar det ett par dagar för warfarin att ge effekt?
  • warfarin är en kompetativ inhibitor till vitamin K
  • IIa, II, X annat ord för trombin
  • II, IIa, IX, V annat ord för protrombin
  • LMWH inhiberar bara Xa (inte den & IIa) och kräver inte labb monitoring skillnad mellan Low Molecular Weight Heparins(LMWH) och Heparin
  • injektion, increasing the effect of antithrombin III (AT III) likheter mellan Low Molecular Weight Heparins(LMWH) och Heparin
  • calcium antagonists, nitrates typer av drugs för att direkt påverka BP (genom contractile function i smooth muscle)
  • ACE inhibitors, AT I receptor antagonists, a1-adrenoreceptor antagonist typer av drugs för att indirekt påverka BP (genom system som påverkar contraction i smooth muscle)
  • Angiotensin-converting enzyme (ACE) inhibitors inhiberar produktion av angiotensin II från angiotensin I
  • AT I receptor receptor som angiotensin II acts on
  • AT I receptor antagonists, ARB, angiotensin II type 1 receptor blocking blocking angiotensin II from activating vascular smooth muscle to constrict
  • 1st generation beta blockers non selective beta blockers
  • 2nd generation beta blockers beta 1 selective blockers
  • APC atingen presenting cell
  • allergy type 1 IgE antibody -> runt i kroppen -> binder till inflammatory cells
  • inflammatory mediators messenger acts on blodkärl/cells to promote an inflammatory response(tex Leukotrienes,cytokines, histaminer)
  • Leukotrienes och olika cytokines vanliga inflammatory mediators i lower airways
  • viktigt vid treatment av astma relax smooth muscle OCH underlying inflammation
  • vanliga Broncho-dilating drugs är Adrenergic β2 agonister
  • Glucocorticoids Anti-inflammatory drugs vid Pharmacological treatment of Asthma
  • short acting beta2 agonister är mindre lipofila än long acting och kommer därför inte stanna i membranet lika länge
  • det finns risk för Desensitization om LABA (long acting beta2 agonister) används istället för SABA som används vid acute problems
  • drf är anti-ACh viktigt vid astma ACh skapar smooth muscle contraction och ökad slem produktion
  • mab monoclonal antibody
  • innate immune system ospecifikt försvar. första skyddet mot mikrobes. barriärer & phagocytes
  • adaptive immune system specifikt försvar. kropper reagerar på triggers ->skapar antibodies. b & t lymfocyter
  • Active immunization disease organism triggers immune system to produce antibodies (tex vaccination)
  • Passive immunization person får färdiga antikroppar för en sjukdom (tex serumbehandling)
  • bactericidal-agents, bacteriostatic-agent antibiotika som minskar antalet viable bacteria för att de dör
  • bacteriostatic agent, bactericidal agents antibiotica minskar nr viable bacteria via bacteria growth arrest
  • acquired resistance due to: altered targets, decreased accumulation, enzymatic inactivation
  • many antibiotics acts on the cellwall of the bacteria. good since eukaryotes are lacking this
  • β-lactam antibiotika antibiotika som inhibit Penicillin-binding protein(PBP) detta inhibit cell wall syntesis (tex penicillin)
  • β-lactamase inhibitors use with β-lactam antibiotika to overcome antibiotika resistance
  • β-lactamase enzyme attacks β-lactam ring på antibiotikan
  • 3 steg Chemotherapeutic treatment compounds must reach cells, stop cell dividing, apoptosis
  • When do we need antiinflammatory drugs? defensive response acting inappropriatly(allergi) or Symptom relief
  • NSAID (COX-inhibitors), Glucocorticoids, Anti-histamines, Anti-cytokines, MABs Anti-inflammatory drug i form av enzyme inhibitors
  • Glucocorticoids, Anti-cytokines, MABs, NSAID (COX-inhibitors) Anti-inflammatory drug i form av Transcription modulator
  • antipyretic drugs drugs för att minska feber
  • analgesic drugs smärtstillande läkemedel
  • NSAIDs (non-steroidal anti-inflammatory drugs) COX inhibitors: anti-inflammatory, antipyretic and analgetic effect
  • COX 1 ivävnder, normal funktion, påverkar njuren, mag/tarm, TXA2
  • COX 2 induceras vid inflammation, medierar inflammatoriska responser
  • vad gör ASA med platelets? acetylerar COX som blir inaktivt. platelets saknar nucleus så kan inte prodcuera mer COX
  • COX 1 har mindre substrate channel än COX 2. varför är det bra? stora drugs påverkar bara cox2. bra i anti-inflammatory drugs
  • annexin upregulated by GC. inhiberar phospholipase A2. ↓ inflammation
  • Anti-inflammatory drugs drugs reduce inflammation
  • Immunosuppressive drugs drugs affect the immune system – reduce the amount and/or action of the T and B cells.
  • L01B, L01A, L01C, L01X Anti-metabolites (Pyrimidine-. Purineanalogous-. Folic acid analogous)
  • L01A, L01B, L01X, L01C Alkylating agents and platina compounds
  • L01C, L01A, L01B, L01D Plant alkaloids and other natural products (mitos inhibitor/ Cell division inhibitors)
  • L01D, L01X, L01A, L01B Cytotoxic antibiotics and related drugs (Topoisomerase inhibitors)
  • L01X, L01B, L01C, L01D Other anti neoplastic agents(tex Proteinkinase inhibitors. Monoclonal antibodies. Sensitizing agents for radiation)
  • receptor-internalization, internalization receptorer moves från membran till inuti cellen
  • unionized, ionized har lättast att passera membran
  • Anti-histamines, NSAID(COX-inhibitors), Glucocorticoids Anti-inflammatory drug i form av Receptor antagonists
  • högre half-life, lägre half-life, oförändrar half-life hög vd innebär att det mesta av drugsen har lämnat bloodstream-Resulterar i

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