Smärta/rörelseapparaten - vanliga LM Flashcards
morfin
Läkemedelsgrupp: narkotiskt analgetikum
Substansnamn: morfin
Beskrivning: the principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle. In January, 2017, morphine was approved for the treatment of chronic pain.
Verkningsmekanism: The precise mechanism of the analgesic action of morphine is unknown. However, specific CNS opiate receptors have been identified and likely play a role in the expression of analgesic effects. Morphine first acts on the mu-opioid receptors. The mechanism of respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to increases in carbon dioxide tension and to electrical stimulation. It has been shown that morphine binds to and inhibits GABA inhibitory interneurons. These interneurons normally inhibit the descending pain inhibition pathway. So, without the inhibitory signals, pain modulation can proceed downstream.
Indikation: Svåra smärttillstånd.
oxykodon
Läkemedelsgrupp: Naturliga opiumalkaloider, opiater
Substansnamn: Oxikodon
Beskrivning: Oxycodone is a semisynthetic derivative of codeine that acts as a narcotic analgesic more potent and addicting than codeine. An extended-release (ER) form of oxycodone (Xtampza ER) was approved for the management of daily, around-the-clock pain management in April, 2016.
Verkningsmekanism: Oxycodone acts as a weak agonist at mu, kappa, and delta opioid receptors within the central nervous system (CNS). Oxycodone primarily affects mu-type opioid receptors, which are coupled with G-protein receptors and function as modulators, both positive and negative, of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine, and noradrenaline is inhibited. Opioids such as oxycodone also inhibit the release of vasopressin, somatostatin, insulin, and glucagon. Opioids close N-type voltage-operated calcium channels (kappa-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (mu and delta receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
Indikation: Svår smärta som endast kan behandlas adekvat med opioidanalgetika.
fentanyl
Läkemedelsgrupp: Analgetikum
Substansnamn: Fentanyl
Beskrivning: A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance.
Verkningsmekanism: Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. Fentanyl’s analgesic activity is, most likely, due to its conversion to morphine. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hypopolarization and reduced neuronal excitability.
Indikation:
Vuxna: Produkten är avsedd för behandling av kronisk svårbehandlad smärta orsakad av cancer. Behandling av kronisk svårbehandlad smärta.
Barn: Produkten är avsedd för långtidsbehandling av svår kronisk smärta hos barn från 2 års ålder som får opioidbehandling.
paracetamol
Läkemedelsgrupp: Analgetikum, antipyretikum
Substansnamn: Paracetamol
Vanliga märken: Alvedon, Pamol, Citodon och Panodil
Beskrivning: Acetaminophen, also known as paracetamol, is commonly used for its analgesic and antipyretic effects. Its therapeutic effects are similar to salicylates, but it lacks anti-inflammatory, antiplatelet, and gastric ulcerative effects.
Verkningsmekanism: Acetaminophen is thought to act primarily in the CNS, increasing the pain threshold by inhibiting both isoforms of cyclooxygenase, COX-1, COX-2, and COX-3 enzymes involved in prostaglandin (PG) synthesis. Unlike NSAIDs, acetaminophen does not inhibit cyclooxygenase in peripheral tissues and, thus, has no peripheral anti-inflammatory affects. While aspirin acts as an irreversible inhibitor of COX and directly blocks the enzyme’s active site, studies have found that acetaminophen indirectly blocks COX, and that this blockade is ineffective in the presence of peroxides. This might explain why acetaminophen is effective in the central nervous system and in endothelial cells but not in platelets and immune cells which have high levels of peroxides. Studies also report data suggesting that acetaminophen selectively blocks a variant of the COX enzyme that is different from the known variants COX-1 and COX-2. This enzyme is now referred to as COX-3. Its exact mechanism of action is still poorly understood, but future research may provide further insight into how it works. The antipyretic properties of acetaminophen are likely due to direct effects on the heat-regulating centres of the hypothalamus resulting in peripheral vasodilation, sweating and hence heat dissipation.
Indikation: Huvudvärk, tandvärk, feber vid förkylningssjukdomar, menstruationssmärtor, muskelsmärtor, som analgetikum vid reumatiska smärtor, hyperpyrexi.
sumatriptan
Läkemedelsgrupp: Selektiva 5-HT1 receptoragonister.
Substansnamn: Sumatriptan
Beskrivning: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of migraine disorders. A transdermal patch version of sumatriptan is currently in phase I trials in the U.S.
Verkningsmekanism: The 5-HT1B and 5-HT1D receptors function as autoreceptors, which inhibit the firing of serotonin neurons and a reduction in the synthesis and release of serotonin upon activation. After sumatriptan binds to these receptors, adenylate cyclase activity is inhibited via regulatory G proteins, incrases intracellular calcium, and affects other intracellular events. This results in vasoconstriction and inhibtion of sensory nociceptive (trigeminal) nerve firing and vasoactive neuropeptide release.
Indikation: Sumatriptan tabletter är avsedda för akut behandling av migränattacker med eller utan aura. Sumatriptan ska endast användas när migrändiagnosen är helt säkerställd.
allopurinol
Läkemedelsgrupp: Medel som hämmar produktionen av urinsyra.
Substansnamn: Allopurinol
Beskrivning: A xanthine oxidase inhibitor that decreases uric acid production. It also acts as an antimetabolite on some simpler organisms.
Verkningsmekanism: Allopurinol and its active metabolite, oxypurinol, inhibits the enzyme xanthine oxidase, blocking the conversion of the oxypurines hypoxanthine and xanthine to uric acid. Elevated concentrations of oxypurine and oxypurine inhibition of xanthine oxidase through negative feedback results in a decrease in the concentrations of uric acid in the serum and urine. Allopurinol also facilitates the incorporation of hypoxanthine and xanthine into DNA and RNA, leading to a feedback inhibition of de novo purin synthesis and a decrease in serum uric acid concentrations as a result of an increase in nucleotide concentration.
Indikation:
Vuxna
Alla former av hyperurikemi som inte kan kontrolleras med diet inkluderat sekundär hyperurikemi av varierande ursprung samt vid kliniska komplikationer av tillstånd av hyperurikemi, särskilt manifesterad gikt, uratnefropati och för upplösande och förebyggande av njursten.
Behandling av återkommande blandade kalciumoxalatstenar vid samtidig hyperurikemi, när vätske-, diet- och liknande åtgärder misslyckats.
Endast Alluporinol Orion 100 mg tabletter:
Barn och ungdomar
Sekundär hyperurikemi av varierande ursprung.
Urinsyranefropati under behandling av leukemi.
Ärftliga enzymbristsjukdomar, Lesch-Nyhan-syndromet (partiell eller total hypoxanthin-guanin-fosforibosyltranferas-brist) och adeninfosforibosyltransferas-brist.
diklofenak
Läkemedelsgrupp: Antiflogistikum med analgetisk och antipyretisk effekt
Substansnamn: Diklofenak
Beskrivning: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.
Verkningsmekanism: The antiinflammatory effects of diclofenac are believed to be due to inhibition of both leukocyte migration and the enzyme cylooxygenase (COX-1 and COX-2), leading to the peripheral inhibition of prostaglandin synthesis. As prostaglandins sensitize pain receptors, inhibition of their synthesis is responsible for the analgesic effects of diclofenac. Antipyretic effects may be due to action on the hypothalamus, resulting in peripheral dilation, increased cutaneous blood flow, and subsequent heat dissipation.
Indikation: Reumatoid artrit. Artros. Mb. Bechterew. Dysmenorré utan organisk orsak.
ibuprofen
Läkemedelsgrupp: Icke-steroida antiinflammatoriska/antireumatiska medel, NSAID
Substansnamn: Ibuprofen
Vanliga namn: Ipren, ibumetin
Beskrivning: Ibuprofen, a propionic acid derivative, is a prototypical nonsteroidal anti-inflammatory agent (NSAIA) with analgesic and antipyretic properties.
Verkningsmekanism: The exact mechanism of action of ibuprofen is unknown. Ibuprofen is a non-selective inhibitor of cyclooxygenase, an enzyme invovled in prostaglandin synthesis via the arachidonic acid pathway. Its pharmacological effects are believed to be due to inhibition cylooxygenase-2 (COX-2) which decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever and swelling. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation. Inhibition of COX-1 is thought to cause some of the side effects of ibuprofen including GI ulceration. Ibuprofen is administered as a racemic mixture. The R-enantiomer undergoes extensive interconversion to the S-enantiomer in vivo. The S-enantiomer is believed to be the more pharmacologically active enantiomer.
Indikation: Mild till måttlig smärta såsom huvudvärk, inklusive migränhuvudvärk, tandvärk. Primär dysmenorré. Feber. Reumatiska tillstånd såsom artrit (t ex reumatoid artrit inklusive juvenil reumatoid artrit), degenerativa artrittillstånd (t ex artros), icke-artikulära reumatiska tillstånd, andra muskel- och ledsyndrom och mjukdelsskador.
naproxen
Läkemedelsgrupp: Antiflogistikum med analgetisk och antipyretisk effekt
Substansnamn: naproxen
Beskrivning: An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout.
Verkningsmekanism: The mechanism of action of naproxen, like that of other NSAIDs, is believed to be associated with the inhibition of cyclooxygenase activity. Two unique cyclooxygenases have been described in mammals. The constitutive cyclooxygenase, COX-1, synthesizes prostaglandins necessary for normal gastrointestinal and renal function. The inducible cyclooxygenase, COX-2, generates prostaglandins involved in inflammation. Inhibition of COX-1 is thought to be associated with gastrointestinal and renal toxicity while inhibition of COX-2 provides anti-inflammatory activity.
Indikation: Reumatoid artrit. Juvenil reumatoid artrit. Artros. Mb Bechterew. Dysmenorré utan organisk orsak. Akuta anfall av migrän. Akuta smärttillstånd av lätt till måttlig intensitet.
tramadol
Läkemedelsgrupp: Analgetikum
Substansnamn: tramadol
Beskrivning: A narcotic analgesic proposed for moderate to severe pain. It may be habituating. [PubChem] Tramadol is also prepared as a variable release capsules, marketed under the brand name ConZip. For example, a 150 mg capsule will contain 37.5 mg of the immediate release form and 112.5 mg of the extended release form.
Verkningsmekanism: Tramadol and its O-desmethyl metabolite (M1) are selective, weak OP3-receptor agonists. Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. The analgesic properties of Tramadol can be attributed to norepinephrine and serotonin reuptake blockade in the CNS, which inhibits pain transmission in the spinal cord. The (+) enantiomer has higher affinity for the OP3 receptor and preferentially inhibits serotonin uptake and enhances serotonin release. The (-) enantiomer preferentially inhibits norepinephrine reuptake by stimulating alpha(2)-adrenergic receptors.
Indikation: Behandling av måttlig till svår smärta.
alendronat
Läkemedelsgrupp: Bisfosfonat, för behandling av skelettsjukdomar
Substansnamn: alendronsyra
Beskrivning: Alendronic acid (alendronate) is a nitrogen-containing, second generation bisphosphonate. Bisphosphonates were first used to treat Paget’s disease in 1971. This class of medications is comprised of inorganic pyrophosphate analogues that contain non-hydrolyzable P-C-P bonds. Similar to other bisphosphonates, alendronate has a high affinity for bone mineral and is taken up during osteoclast resorption. Alendronate inhibits farnesyl pyrophosphate synthetase, one of the enzymes in the mevalonic acid pathway involved in producing isoprenoid compounds that are essential for post-translational modification of small guanosine triphosphate (GTP)-binding proteins, such as Rho, Ras and Rab. Inhibition of this process interferes with osteoclast function and survival. Alendronate is used for the treatment of osteoporosis and Paget’s disease.
Verkningsmekanism: The action of Alendronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Alendronate also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates (such as pamidronate, alendronate, risedronate, ibandronate and zoledronate) appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting FPP synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass.
Indikation: Behandling av postmenopausal osteoporos. Alendronat minskar risken för kot- och höftfrakturer.
