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What is the pharmacokinetic distribution formula?
Amount of drug in body / [drug in plasma]
What is the pharmacokinetic elimination formula?
- In general it takes 4-5 half-lives for complete drug removal from body
What are first order rate kinetics?
Elimination = 0.69(distribution)/x half-lives
What are zero order rates?
- No half life
- Concentration vs time
What does potency mean?
Amount of drug required to produce an effect
What does efficacy mean?
Effect of drug once it is bound
What does affinity mean?
What does cholinergic mean?
What does adrenergic mean?
What cholinergic receptors are in the eye?
- Iris sphincter causing miosis
- Ciliary muscle causing accommodation
- Lacrimal gland causing increased tear production
What adrenergic receptors are in the eye?
- Iris dilator, a1, causing dilation
- TM, b2, causing increased outflow
- Ciliary muscle, b2, causing relaxation of accommodation
- NPCE,b1 b2, increases aqueous formation
- CB vasculature, a2, reduces aqueous formation
What alpha receptors are found in the eye?
- Iris dilator (a1)
- CB vasculature (a2)
What beta receptors are found in the eye?
- TM (b2)
- Ciliary muscle (b2)
- NPCE (b1, b2)
What direct acting Cholinergic Agonists are there?
What indirect acting cholinergic agonists are there?
- neostigmine - MG
What cholinergic antagonists are there (and their order of strength)?
- Botulina toxin
What autonomic nervous system acts on nicotinic and muscarinic receptors?
What is the MOA of pilocarpine?
- Stimulates longitudinal muscle of ciliary body
- Secondarily opens up trabecular spaces
What are main side effects of pilocarpine?
- Myopic shifts
- Retinal detachments
How do indirect cholinergic agonists work?
What drug is the DOC for tx for MG?
What drug is used to diagnosis MG?
What is echothiophate used for?
Diagnosis ant tx for accommodative esotropia
What is the MOA for cholinergic antagonists?
- They STopACH
How long do each cholinergic antagonist drug work?
- Atropine (7-10 days mydriatic)/(7-12 days cycloplegic)
- Scopolamine (3-7 days mydriatic)/(5-7 days cycloplegic)
- Homatropine(1-3 days mydriatic /cycloplegic)
- Cyclopentolate (24hrs mydriatic/cycloplegic)
- Tropicamide (4-6 hours mydriatic)/(4 hrs cycloplegic)
What is atropine use for?
- Tx of uveitis
- Breaking synechiae
- Amblyopia tx
In what patient demographic is atropine contraindicated
What is homatropine used for?
Anterior uveitis to minimize pain
What ocular adrenergic agonists are there?
- Naphazoline (naphcon)
- Tetrahydrozoline (visine)
What is hydroxyamphetamine used for?
- Determines location of horner's syndrome
- Used after cocaine or apraclonidine
What receptor is acted on by apraclonidine and brimonidine
What is the effect of apraclonidine and brimonidine?
- Decrease aqueous humor production
- Increase uveoscleral outflow
What is the brand name for apraclonidine?
What percentage of IOP reduction is expected with apraclonidine?
Why isn't apraclonidine used as a regular long-term glaucoma medication?
- Not effective in chronic therapy (tachyphylaxis)
- High allergic response in long-term therapy
What is apraclonidine used for?
- Acute IOP reduction
- Diagnosis horner's syndrome instead of cocaine
- There is no effect on the normal pupil
What is the brand name for brimonidine?
What glaucoma drop also causes follicular conjunctivitis?
What other drugs (of interest) cause adverse reactions with brimonidine?
What are contraindications for using ocular epinephrine?
- Not used in aphakes due to risk of CME
- Not used in narrow angles due to angle closure
- Cardiovascular disease
what drugs are systemic adrenergic agonists
what systemic/ocular classes of drugs are in the adrenergic antagonist family?
What are the systemic side effects of beta blockers?
- CNS -disorientation, depression, fatigue
- Cardiovascular- bradycardia, arrhythmias, syncope
- Pulmonary - dyspnea, wheezing, bronchospasm
- Digestive - nausea, vomiting, diarrhea, abdominal pain
- Reproductive - impotence
What alpha blocker can cause floppy iris syndrome?