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36 Cards in this Set
- Front
- Back
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What is Naltrexone used for?
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Reducing craving in Alcohol dependence
Poor outcomes for opioid dependancy management |
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What is Naloxone used for?
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Reversal of OD
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How does alcohol produce it's effects?
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Decrease NMDA activity
Decreased voltage gated Ca channel activity Increase GABA-a activity |
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How do opioids produce their effects?
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Decrease Ca entry - therefore decrease neurotransmitter release
Increase K exit further polarising the cell - therefore decrease neurotransmitter release Inactivate AC therefore decrease cAMP - therefore decrease neurotransmitter release |
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Where are CB receptors located?
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Presynaptically. Inactivate AC leading to decreased cAMP, and inhibits Ca entry.
Decreased transmitter release over all |
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How does cocaine work?
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Inhibites monoamine re-uptake thereby increaseing 5-HT, NA, DA
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How does heroin work?
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More lipophilic than morphine therefore greater rush. Is an opiate therefore acts on Ca channels, K channels and AC.
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What are 9 outcomes of opiates?
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Constipation
Constricted pupils Cough impaired Analgesia Euphoria - mu Dysphoria - kappa Physical dependance Nausea/Vomiting Respiratory depression |
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What are the 5 types of Adverse Drug Reactions?
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Augmented, Bizzare, Chronic, End, Delayed
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What is the formula for clearance of a drug?
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V of drug cleared by time =
Maintainance dose/Plasma conc |
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How is bioavailability calculated?
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Bioavailability =
Fraction absorbed x fraction that makes it through the liver |
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How is Heparin activity measured?
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APTT
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How do NSAIDS work?
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Inhibit COX which produces Prostaglandins.
COX2 = PG's mediate pain, inflammation and fever. Vasodilation, inhibit platelet aggregation COX1 = Protective and Thromboxane therefore platelet aggregation |
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What are some Glucocorticosteroids?
What are Mineralocorticosteroids? |
Mineralo's effect water balance and electrolytes
Gluco effect inflam, metab. Aldosterone (M) Cortisol (1:1 G:M) Prednisone (synthetic - 4 tims more G than M) Dexamethasone (30 times G) |
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How do Glucocorticosteroids work?
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Inhibit inflammation of the DNA level:
Activate transcription of anti-inflam proteins eg Annexin Destabilises inflam mRNA by binding stabilising proteins Deactivates Histone Acetylases and Activates Histone Deacetylases for pro-inflam genes therefore DNA wound ip |
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Why do MOR mediate euphoria and KOR dysphoria?
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MORs inhibit a GABA neuron that normally inhibits a Dopamine releaseing neuron running from the VTA to the NA
KOR are found ON this dopamine releasing neuron in the NA - thus it inhibits DA release |
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The opiate precurser Proenkaphalin provides which endogenous opiates and where?
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leu and met enkaphalin.
Nerve cells, PAG and Adrenal Medulla |
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The opiate precurser Prodynorphin provides which endogenous opiates and where?
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A & B Dynorphin, alpha Dynorphin
Nerve cells only |
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The opiate precurser Proopiomelanocortin provides which endogenous opiates and where?
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beta endorphin, ACTH
Nerve cells and Brain |
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How is pain transmitted?
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Nociceptors
Peripheral nerves Dorsal Horn of Spinal cord Dorsal Horn of Spinal cord PAG PAG Thalamus SomatoSENSORY cortex - Sensation Anterior Cingulate Gyrus - Emotion |
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How do Opioids interfer with Prostaglandins?
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PG increase AC, sensitising nociceptors to Histamines to mediate pain.
Opioids do the opposite. |
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How do NSAIDS and Opioids act synergistically?
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BOTH decrease AC in nociceptors (NSAIDS decrease PG production and Opioids decrease PG effects via AC)
NSAIDs block the use of Arachidonic acid by COX. THus more Arachidonic acid for use in Opiates Lipoxygenase pathway that leads to K expulsion therefore hyperpolarised membrane. GABA release inhibited. |
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How do opioids activate the descending pathway?
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Descending circuit normally inhibited by GABA interneuron. Opioid inhibits this, thus the desending pathway is activated and pain is not sent up!
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Out of NABCOP which have the worst withdrawal?
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Opioids, Alcohol, Benzodiazapines
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Out of NABCOP which have the worst craving?
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Opioids, Nicotine, Psychostimulants
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Out of NABCOP which have the worst tolerance?
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Opioids
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Which drugs will cause placental abruption in pregnancy?
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Cocaine and ICE
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How might opioid tolerance occur?
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Phophorylation of the activated G-protein receptor leading to internalisation
Upregulation of AC via CREB |
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Which drugs have the most dangerous withdrawal?
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Alcohol and Benzos due to seizures
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What is the action of Salbutamol?
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Relax smooth muscle via beta2
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When are bisphosphonates used and how do they work?
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For osteoporosis, pagent's disease, bone metastisis.
Ingested by Osteoclast then killed |
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What are some bisphosphonates
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Alendronate
Risendronate |
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Uricase treats what and how?
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Gout
Makes uric acid to water soluble Allantoin - dissolves tophi |
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Urosurics treat what and how?
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Block reabsorption of uric acid BUT causes Renal Canaliculi
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What blocks Xanathine Oxidase and why would you want to?
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Allopurinol and Febuxostat
Decrease uric acid production |
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What drugs cause fibrosis?
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Bleomycin
Nitrofurantoin Amiodarone |
