Farmakokinetika Osnovni principi, absorpcija zdravil
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1 Farmakokinetika Osnovni principi, absorpcija zdravil Lovro Stanovnik Inštitut za farmakologijo in eksperimentalno toksikologijo Medicinska fakulteta, Univerza v Ljubljani
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3 Osnovna farmakokinetska dogajanja (ADME) Absorpcija zdravila z mesta aplikacije Porazdelitev po telesu (distribucija) Metabolizem (biotransformacija) Izločanje iz organizma (ekskrecija, eliminacija)
4 Faktorja, ki vplivata na koncentracijo zdravila na mestu delovanja Organizem sestavljen iz več predelkov (kompartmentov) enakomerna porazdelitev zdravila enaka koncentracija oprehajanje molekul zdravila okemijska transformacija.
5 Prehajanje zdravil v organizmu Prenašanje s topilom (pretok krvi) pomembno pri časovnem poteku razporeditve zdravil. Difuzija (posamezne molekule, kratke razdalje) pomembna pri prehajanju zdravil preko barier, ki ločujejo telesne kompartmente
6 Bariere med kompartmenti Med znotrajcelično in zunajcelično tekočino celična membrana Epitelne bariere (črevo, ledvice) dve celični membrani Endotel žil razlike med organi: Pore med celicami proteinski matriks filter Placenta in OŽ med endotelnimi celicami tesni stiki + periciti zelo omejena permeabilnost Jetra, vranica, endokrine žleze pore med endotelnimi celicami fenestriran endotel Postkapilarne venule specializirana funkcija migracija levkocitov
7 Prehajanje zdravil preko celičnih membran Direktna difuzija skozi plasti lipidov. Difuzija skozi vodne pore posebni transmembranski proteini ('akvaporini ). Vezava na transmembranski prenašalni protein sprememba konformacije sprostitev na drugi strani membrane. Pinocitoza.
8 Figure 7-1 Routes by which solutes can traverse cell membranes. (Molecules can also cross cellular barriers by pinocytosis.) Downloaded from: StudentConsult (on 26 February :43 PM) 2005 Elsevier
9 Prehajanje zdravil preko lipidnih membran Nepolarne molekule večinoma topne v lipidih prehajanje odvisno od: koncentracijskega gradienta koeficienta permeabilnosti pretežno določen s porazdelitvenim koeficientom: topnost v lipidih topnost v vodi večina zdravil slabe kisline ali baze za topnost v lipidih pomembna stopnja disociacije nedisociiran del večinoma dobro topen v lipidih.
10 Figure 7-2 The importance of lipid solubility in membrane permeation. Figure shows the concentration profile in a lipid membrane separating two aqueous compartments. A lipid-soluble drug (A) is subject to a much larger transmembrane concentration gradient (ΔCm) than a lipid-insoluble drug (B). It therefore diffuses more rapidly, even though the aqueous concentration gradient (C1-C2) is the same in both cases. Downloaded from: StudentConsult (on 26 February :43 PM) 2005 Elsevier
11 ph in stopnja ionizacije Za šibko bazo velja: K a BH B H in: pk a = ph + log 10 BH B (Henderson Hasselbachova enačba) +
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13 Figure 7-3 Theoretical partition of a weak acid (aspirin) and a weak base (pethidine) between aqueous compartments (urine, plasma and gastric juice) according to the ph difference between them. Numbers represent relative concentrations (total plasma concentration = 100). It is assumed that the uncharged species in each case can permeate the cellular barrier separating the compartments, and therefore reaches the same concentration in all three. Variations in the fractional ionisation as a function of ph give rise to the large total concentration differences with respect to plasma. IONIC TRAPPING Downloaded from: StudentConsult (on 26 February :43 PM) 2005 Elsevier
14 Posledice vpliva ph na porazdelitev zdravil Nakisanje urina pospeši izločanje šibkih baz in upočasni izločanje šibkih kislin. Naalkaljenje urina ima nasproten učinek. ph plazme (npr. z Na bikarbonatom) prehajanje šibke kisline iz OŽ v plazmo. ph plazme (npr. z inhibitorjem karbonske anhidraze, acetazolamidom) koncentriranje šibke kisline v OŽ (povečanje nevrotoksičnosti) npr. salicilati Sprememba ph urina možnost vpliva na izločanje šibkih kislin oz. baz.
15 Figure 7-4 pka values for some acidic and basic drugs. Downloaded from: StudentConsult (on 26 February :43 PM) 2005 Elsevier
16 Prenašalci Prenos fiziološko pomembnih molekul (sladkorji, aminske kisline, ioni, transmitorji ) Pomen za zdravila, podobna endogenim snovem Facilitirana difuzija v smeri gradienta. Prenos sklopljen z Na + - elektrokemičnim gradientom aktivni transport. Možnost saturacije visoka koncentracija liganda Kompeticija za vezavno mesto
17 Farmakokinetično pomembna mesta s prenašalci Hematoencefalna bariera Gastrointestinalni trakt Ledvični tubuli Biliarni trakt Placenta Glikoprotein P rezistenca na zdravila vloga pri absorpciji in distribuciji številnih zdravil. Lokalizacija: GIT Astrociti ob žilah v možganih Ledvični tubuli Biliarni sistem
18 Vpliv na porazdelitev zdravil Vezava na plazemske beljakovine Porazdelitev v maščevju in drugih tkivih
19 Vezava na plazemske beljakovine Najpomembnejša vezava na plazemske albumine (kisla in nekatera bazična zdravila) vezava na ß-globulin kisli glikoprotein Vezava odvisna od: koncentracije prostega zdravila njegove afinitete za vezavna mesta koncentracije proteinov Merjenje koncentracij običajno: celokupno zdravilo
20 Vezava na plazemske beljakovine Podobne zakonitosti kot pri vezavi zdravila na receptor: D + S DS prosto zdravilo vezavno mesto kompleks Koncentracija albumina v plazmi 0,6 mmol/l (4 g/100 ml) 2 vezavni mesti/molekulo kapaciteta 1,2 mmol/l plazme kapaciteta presega terapevtske koncentracije večine zdravil ni saturacije. Izjeme: tolbutamid, sulfonamidi, fenibutazon..
21 Figure 7-5 Binding of phenylbutazone to plasma albumin. The graph shows the disproportionate increase in free concentration as the total concentration increases, owing to the binding sites approaching saturation. (Data from Brodie B, Hogben C A M 1957 J Pharm Pharmacol 9: 345.) Downloaded from: StudentConsult (on 26 February :43 PM) 2005 Elsevier
22 Porazdelitev v maščevju in drugih tkivih Porazdelitveni koeficient Le malo zdravil dovolj lipofilnih izjema tiopental Majhen pretok krvi skozi maščevje pomen pri dolgotrajni aplikaciji (ksenobiotiki) Nalaganje v drugih tkivih: klorokvin melanin retinopatija tetraciklini kosti in zobje amiodaron jetra in pljuča topnost v lipidih topnost v vodi
23 Osnovna farmakokinetska dogajanja (ADME) Absorpcija zdravila z mesta aplikacije Porazdelitev po telesu (distribucija) Metabolizem (biotransformacija) Izločanje iz organizma (ekskrecija, eliminacija)
24 Absorpcija zdravil Mesta aplikacije Peroralna Sublingvalna Rektalna Aplikacija na druge epitelne površine (koža, kornea, vagina in nazalna mukoza) Inhalacija Injekcija (parenteralna aplikacija): Subkutana Intramuskularna Intravenska Intratekalna.
25 Figure 7-6 The main routes of drug administration and elimination. Downloaded from: StudentConsult (on 26 February :43 PM) 2005 Elsevier
26 Absorpcija ob peroralni aplikaciji Večinoma difuzija skozi lipidne plasti (ph, pk a ); Prenos s prenašalci ( l-dopa, 5-FU, Fe, Ca) Približno 75% peroralno danega zdravila se absorbira v 1-3 urah Faktorji ki vplivajo na hitrost absorpcije: gastrointestinalna motiliteta (zdravila, bol. stanja) pretok krvi skozi splanhnično področje (vplivi) fizikalno kemijski faktorji (interakcije) velikost delcev in oblika zdravila (posebne farmacevtske oblike prirejeno sproščanje, lokalno delovanje).
27 Značilnosti posameznih delov prebavil Usta venska kri mimo jeter hitra pasaža Želodec nizek ph (1 3), možnost razpada zdravila (ph, encimi), hitra pasaža Duodenum, jejunum, ileum ph med 6 in 7, velika absorptivna površina (villi), glavno mesto enteralne absorpcije zdravil Rektum venska kri mimo portalnega obtoka
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30 Figure 7-7 Absorption of drugs from the intestine, as a function of pka, for acids and bases. Weak acids and bases are well absorbed; strong acids and bases are poorly absorbed. (Redrawn from Schanker L S et al J Pharmacol 120: 528.) Downloaded from: StudentConsult (on 2 March :48 PM) 2005 Elsevier
31 Figure 7-4 pka values for some acidic and basic drugs. Downloaded from: StudentConsult (on 26 February :43 PM) 2005 Elsevier
32 Figure 7-8 Variation in oral absorption among different formulations of digoxin. The four curves show the mean plasma concentrations attained for the four preparations, each of which was given on separate occasions to four subjects. The large variation has caused the formulation of digoxin tablets to be standardised since this study was published. (From Lindenbaum J et al N Engl J Med 285: 1344.) Downloaded from: StudentConsult (on 26 February :43 PM) 2005 Elsevier
33 Biološka uporabnost zdravil (bioavailability, F) Delež zdr., ki pride iz prebavil v sistemsko cirkulacijo AUC Konc. zdravila v plazmi konc. i.v. konc. p.o
34 Koncentracija Površina pod krivuljo - AUC Čas
35 Biološka uporabnost zdravila Faktor absorpcije zdravila F = AUC AUC po.. iv.. Biološko uporabnost omejuje: Absorpcija z mesta aplikacije (večinoma peroralna) Metabolizem v črevesni steni oz. v jetrih pred prihodom v sistemsko cirkulacijo (metabolizem prvega prehoda)
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37 Drugi načini aplikacije zdravil APLIKACIJA NA EPITELNE POVRŠINE Kutana aplikacija Nazalni sprayi Očesne kapljice Inhalacija ADMINISTRACIJA Z INJICIRANJEM Metode za zakasnitev absorpcije Intratekalno injiciranje
38 Koža Skozi kožo prehajajo zdravila z difuzijo (zakonitosti difuzije) vplivi: vodotopne molekule v glavnem ne prehajajo stanje kože (nepoškodovana, hiperemična, opekline, rane, vnetja, obliži,...) Kutana aplikacija pomen: za lokalno delovanje za sistemsko delovanje apsorpcija (gliceril trinitrat, estradiol, nikotin, morfin... aplikacija z obliži) možnost absorpcije toksičnih snovi (CCl 4, organska topila, tetraetilsvinec, živo srebro, lokalni anestetiki, organofosfatni insekticidi,...)
39 KOŽA absorpcija, otroci Otroci so posebno dovzetni za neželene učinke snovi! Spreminjanje razmerja med povprečno površino in maso s starostjo Otrok (1 mesec) Otrok (5let) Odrasel Površina [m 2 ] 0,25 0,67 1,9 Teža [kg] 5,0 20,0 70 m 2 /kg x ,4 2,
40 Nazalna aplikacija Snovi z lokalnim učinkom (dekongestivi,. ) Sistemski učinek: Analogi peptidnih hormonov (GnRH, kalcitonin, ) Aplikacija na očesno veznico Lokalno delovanje brez sistemskih učinkov (midriatiki, inhibitorji karboanhidraze); možnost sistemskih učinkov
41 Inhalacija respiratorni sistem Pljuča izpostavljena vplivom: preko vdihanega zraka preko cirkulacije Učinkovito absorbtivno področje Sistemsko delovanje (inhalacijski anestetiki) Lokalno delovanje: na gladko muskulaturo bronhijev na konsistenco bronhialne sluzi pomembna velikost delcev mesto odlaganja možnost sistemskih učinkov.
42 Aplikacija z injiciranjem Intravensko najbolj direkten vnos v centralni kompartment najhitrejši učinek Intradermalno lokalni anestetiki (trajanje učinka, zakasnitev učinka) Intramuskularno ali subkutano: Hitrost vstopa v obtok je omejena z lipidotopnostjo prekrvljenostjo mišic običajno absorpcija v min., lahko pa hitrejša ali počasnejša; depo preparati Intratekalna administracija: lokalni anestetiki, snovi, ki slabo prehajajo v OŽ (aminoglikozidi)
43 Some Characteristics of Common Routes of Drug Administration I ROUTE ABSORPTION PATTERN SPECIAL UTILITY Intravenous Subcutaneous Absorption circumvented Potentially immediate effects Suitable for large volumes and for irritating substances, or complex mixtures, when diluted Prompt, from aqueous solution Slow and sustained, from repository preparations Valuable for emergency use Permits titration of dosage Usually required for high-molecular-weight protein and peptide drugs Suitable for some poorly soluble suspensions and for instillation of slowrelease implants LIMITATIONS AND PRECAUTIONS Increased risk of adverse effects Must inject solutions slowly as a rule Not suitable for oily solutions or poorly soluble substances Not suitable for large volumes. Possible pain or necrosis from irritating substances
44 Some Characteristics of Common Routes of Drug Administration II ROUTE ABSORPTION PATTERN SPECIAL UTILITY Intramuscular Prompt, from aqueous solution Slow and sustained, from repository preparations Suitable for moderate volumes, oily vehicles, and some irritating substances Appropriate for selfadministration (e.g., insulin) LIMITATIONS AND PRECAUTIONS Precluded during anticoagulant therapy May interfere with interpretation of certain diagnostic tests (e.g., creatine kinase) Oral ingestion Variable, depends on many factors Most convenient and economical; usually more safe Requires patient compliance Bioavailability potentially erratic and incomplete
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