Cardiovascular Mindmap
- Created by: Mohsin
- Created on: 08-04-18 12:50
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- Cardio Therapeutics
- Calcium Channel Antagonists
- Bind to calcium channel protein
- Channels: OPEN, RESTING, INACTIVATED
- Vasodilators
- Found: Skeletal, cardiac and SM muscle contraction
- Ischaemic cells tend to have longer action potentials than healthy cells
- Ca channel is open longer - VASOCONSTRICTION
- If a drug is too water soluble it will undergo first pass metabolism and transferred to the kidneys - no systemic effect
- Ca channel is open longer - VASOCONSTRICTION
- Ischaemic cells tend to have longer action potentials than healthy cells
- 1st Gen: Verapamil (Phenylalkylamines) - OPEN channel state
- 1st Gen: Nifedipine (1,4-Dihydropyrines) - OPEN /CLOSED channel state
- 1st Gen: Diltiazem (Benzothiazepine) - OPEN channel state
- 2nd Gen: Felodipine, Isradipine, NIcardipine, Nimodipine
- MOA: Through the phospholipid bilayer, acts on the closed ion channel
- 2nd Gen: Anipamil, Bepirdil
- MOA: hydrophilic pathway through the ion channel
- 1st Gen: Diltiazem (Benzothiazepine) - OPEN channel state
- 1st Gen: Nifedipine (1,4-Dihydropyrines) - OPEN /CLOSED channel state
- 2nd Gen: more selective for vascular SM.
- Henderson-Hasselbalch Equation
- Acidic centres: 100/ (1+antilog (pka - pH)
- Basic centres: 100/ (1+antilog (pH - pka)
- If the ionisation is HIGH the drug will pass the open channel and vice versa
- ACE (angiotensin covering enzyme)
- Ace cleaves the amide bond between PHE and HIS
- For ACE binding site: charged ZN and ARG (to hold in place)
- ACE Inhibitors
- Captopril
- Thiol group will interact with the Zn and then carboxylic acid group will interact will ARG
- Functional group side effects: rash and loss of sensation
- stop therapy
- Pro-drug
- Enalapril and Ramipril
- Pro-drugs
- Centres very ionised = very water soluble
- Require hydrolysis if ester to create the active di-carboxylic acid
- Pro-drugs
- Captopril
- Calcium Channel Antagonists
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