Miotics mydriatics cycloplegics

NERVE SUPPLY
Dilator Pupillae & Sphincter Pupillae

Acetylcholine receptors: muscarinic
and nicotinic
• A number of drugs target acetylcholine
receptors, blockade of these receptors is
associated with anticholinergic
(parasympatholytic) effect, while stimulation
causes activation of cholinergic
(parasympathomimetic) effects.

Receptors Muscarine &
Nicotinic
Muscarinic Cholinergic Receptors:
A toxin with neurologic effects, first isolated from Amanita muscaria (fly agaric) and also
present in some species of Hebeloma and Inocybe.
The quaternary trimethylammonium salt of 2-methyl-3-hydroxy-5-
(aminomethyl)tetrahydrofuran, it is a cholinergic substance whose pharmacologic effects
resemble those of acetylcholine and postganglionic parasympathetic stimulation (cardiac
inhibition, vasodilation, salivation, lacrimation, bronchoconstriction, gastrointestinal stimulation).
Nicotinic Cholinergic Receptors :
•Relating to the stimulating action of acetylcholine and other nicotine-like agents on
autonomic ganglia, adrenal medulla, and the motor end-plate of striated muscle..
Cholinergic:- It means Relating to nerve cells or fibers that employ acetylcholine as
their neurotransmitter..

Receptors Muscarine (Vs)
Nicotinic1) Nicotinic acetyle choline receptors are ligand gated ion channels, where as
mucarinic Ach receptors are G-proteins coupled receptors system.
2) Nicotine is a agonist/ muscarine( a toxin produced by certain mushrooms) is a
agonist.
3) Action of nicotine is fast(1-2msec)/action of muscarinic is slow (100-
250msec).
4) In case of nicotinic Ach receptor, subtypes based on different sub-unit
composition. muscle and neuronal classification/ in case of muscarinic
receptor at least 5 receptors subtype have been described by molecular cloning.
5) In case of nicotinic receptor agonist effects blocked by tubocuranine/ in case of
muscarinic receptor agonist effects blocked by atropine.
6) Nicotinic receptor found at neuro muscular junction of skeletal muscle, on the
post ganglion neurons of the parasympathetic nervous system and on many
neurons on the brain(hypothalamus)/muscarinc receptor found at
neuromuscular junction of cardiac and smooth muscle as well as on glands and
on the post ganglionic neurons of the sympathetic nervous system..

NEURON &
Neuromuscular Junction

Direct & indirect acting
Parasympathomimetic

Miotics
• Miotics are drugs that cause constriction of pupil.
• These are used in t he management of glaucoma’s and the
treatment of esotropias and accommodation insufficiency.
• Types:
– Pilocarpine
– Carbachol
– Phospholine iodide
– Physostigmine sulphate

1. Pilocarpine
• It is direct acting Parasympathomimetic drug, which duplicates
the muscarine effects of acetylcholine, but has no nicotinic
effects.
• (Acetylcholine is an organic chemical that functions in the brain
and body, as a neurotransmitter—a chemical released by nerve
cells to send signals to other cells)
• Pilocarpine stimulates secretory glands and smooth muscles, but
has no effect on striated muscles.
• Pilocarpine Nitrate, a sterile ophthalmic solution is available as
1%, 2%, 4% Drops
• Pilocarpine is effective in the treatment of glaucoma by
improving the facility of outflow (by contraction of ciliary
muscle) and by decreasing aqueous secretion.
• Onset of miosis occurs with in 10-30 Minutes and
• Lasts for 4-8 Hrs following topical application.

• Control of IOP in Angle Closure Glaucoma
• Emergency relief of Mydriasis in an acutely glaucomatous
situation
• To reverse mydriasis caused by a cycloplegic agent
• In the treatment of accommodative strabismus
• Controversial role in the treatment of hyphema.
• After cataract extraction in cases of ICCE
Pilocarpine Indications and Usage

Pilocarpine Contra-Indications and Warnings
Contraindications:
Hypersensitivity to its components
Anterior Uveitis
Warnings:
•Readily absorbed systemically on topical application.
•Excessive application may elicit toxicity symptoms
(Salivation, lacrimation, sweating, nausea, vomiting,
and diarrhea, bronchiolar spasm and pulmonary
edema can occur)
Precautions:
•Pilocarpine has been reported to cause retinal
detachment in individuals with pre-existing retinal
diseases or predisposed to retinal tears. Safety and
effectiveness in children have not been established.

Pilocarpine (Adverse-Reaction and Dosage)
Adverse-Reaction:
Visual blurring due to miosis
Accommodative spasm
Poor Dark adaptiation caused by the failure of the pupil to dilate in reduced
illumination .
Conjunctival hyperemia.
Miotics have been reported to cause lens opacities in suseptible individuals
after prolonged use.
Allergic blepharo-conjunctivitis,
Ocular pseudopemphoigoid
Corneal epitheliall staining and vascularization
Atypical band keratopathy
Iris hyperemia
Epithelial cyst
Dosage and Administration:
•To aid in emergency Miosis, 1 to 2 drops of one of the
higher concentraitons should be used.
•In reverse mydriasis used depends up on the cycloplegic
used.
•The drops are used bd(every day) – qid (quater in die (four
times a day) in the treatment of angle closure glaucoma.

2. Carbachol
•It is cholinergic prepared as a sterile topical ophthalmic solution
•Carbachol is a direct acting parasympathomimetic that is
sometimes used when allergy or resistance to Pilocarpine
develops.
•Unlike pilocarpine, carbachol has both NICOTINIC and
MUSCARINE actions.
•it is available as 0.75% to 3% Drops
Clinical Pharmacology :
It is a cholinergic (parasympathomimetic) agent.
Carbachol has a double action, it not only stimulates the
motor end plate of the muscle cell, as do all cholinesterase,
but it also partially inhibits cholinesterase.
***Cholinesterase inhibitors are used to reduce the
action of cholinesterase, thereby making more
acetylcholine available to nerve cells in the brain.***

Cholinesterase :
Cholinesterase or choline esterase, which serve as neurotransmitters.
Thus, it is either of two enzymes that catalyze the hydrolysis of these cholinergic
neurotransmitters, such as breaking acetylcholine into choline and acetic acid.
These reactions are necessary to allow a cholinergic neuron to return to its resting
state after activation (For example, in muscle contraction, acetylcholine at a
neuromuscular junction triggers a contraction; but for the muscle to relax
afterward, rather than remaining locked in a tense state, the acetylcholine must be
broken down by a choline esterase).
The main type for that purpose is acetylcholinesterase (also called choline
esterase or erythrocyte cholinesterase)
it is found mainly in chemical synapses and red blood cell membranes.
Cholinesterase

Carbachol Indications and Contraindications
Indications:
For lowering IOP in the Glaucoma
Contraindications:
•Miotics are contraindicated where constriction is
undesirable such as acute iritis.
•Patient showing hypersensitivity to any component to
this preparation.
Warnings:
•Topical only not for injection
•Carbachol should be used with caution in the presence of
corneal abrasion to avoid excessive penetration that can be
produce systemic toxicity and in patients with acute cardiac
failure, bronchial asthma, active peptic ulcer, hyperthyroidism,
gastrointestinal spasm, urinary tract obstruction and
Parkinson's disease.
•As with all Miotics retinal detachment has been reported
when used in certain susceptible individuals

Carbachol Precautions & Adverse Reaction & Dosage
Precautions:
Avoid over dosage
The miosis usually causes difficulty in dark adaptation
Patient should be advised to exercise caution in night driving and
other hazardous occupations in poor light
Adverse reactions:
•This preparation is cable of producing systemic symptoms of a
cholinesterase inhibitor even when the epithelium is intact.
•Transient ciliary and Conjunctival injection, headache and
ciliary spasm with resultant temporary decrease of visual acuity
may occur.
•Salivation, syncope, cardiac arrhythmia, gastrointestinal
cramping, vomiting, asthama and diarrhoea may occur..
•Patient showing hypersensitivity to any component to this
preparation.
Dosage and Administraion:
•It is administrated 3 to 4 times per day

It is available in the following concentrations: 0.03 %, 0.06%, 0.125%, 0.25%
it is a long acting cholinesterase inhibitor for topical use that enhances the effect of
endogenously liberated acetylcholine of iris, ciliary muscle and other
parasympatheticallly innervated structured of the eye.
**** Cholinesterase inhibitors are used to reduce the action of
cholinesterase, thereby making more acetylcholine available to nerve cells
in the brain.
It thereby causes miosis, increase in facility of aqueous humor, fall in intra ocular
pressure and potentiation of accommodation.
Indications and Uses:
IN glaucoma-Chronic open angle glaucoma, sub-acute or chronic angle closeure
glaucoma after iridectormy or where surgery is refused or contraindicated.
Contraindications:
 Active Uveal inflammation
Most cases of angle closure glaucoma due to the possiblity of incresing angle block.
Hypersensitivity to the active or inactive ingredients.
3. Phospholine iodide

ADVERSE REACTIONS:-
 Stinging, burning, lacrimation, lid muscle twitching, conjunctival and ciliary
redness, browache, induced myopia with visual blurring may occur.
Iris cysts may form and, if treatment is continued, may enlarge and obscure
vision. This occurrence is more frequent in children.
Prolonged use may cause Conjunctival thickening, obstruction of nasolacrimal
canals.
Lens opacities, paradoxical increase in intraocular pressure.
 Early chronic glaucoma, 0.03% instilled twice a day. Refrigerated aqueous
solution shows a drop in potency within four weeks.
Adverse Reaction & Dosage

4. Physostigmine Sulphate
•It is an alkaloid obtained from the seeds of physosigmine
venenosum.
•It is an indirectly acting parasympathomimetic agent.
•It is available as a solution 0.25%, 0.5% and an ointment
containing 2 % of the drug.
•It is a reversible anticholine–esterase.
•The mechanism of action involves inhibition of choline
esterase with consequent accumulation of acetylcholine a
the neuromuscular junctions.
Indications:
It can be used in conjunction with pilocarpine in the
treatment of acute glaucoma and angle closure glaucoma
and in diagnosis and treatment of myasthenia gravis.

4. Physostigmine Sulphate
•Contra-indications:
•Predisposing to Retinal Detachment and Hypersensitivity
to the Drug
•Adverse Reactions:
•Twitching (Sudden muscle Spasm)
•Irritation
•Allerginc Reaction
•Depigmentaiton of the lid
•Skin has been noted in some patient with the use as an
ointment
It is administered every 4 to 6 hours.

Mydriatics
•Mydriatics are drugs that cause dilation of pupil (No
cycloplegic effect)
•Phenylephrine Hydrochloride:
•It is available in 5% and 10%
•it is primarily a direct acting drug that stimulates the alpha-
receptors of those structures innervated by the post ganglionic
sympathetic nerve fibers.
•It also causes blanching of the conjunctival vessels
•It is a mydriatic with no cycloplegic effect

Phenylephrine Hydrochloride-
Indications
•Indications and Uses:
•Although the mydriasis produced by 2.5% phenylephrine alone is
generally adequate for detailed examination of the retinal periphery, it is
often sufficient for viewing the posterior pole.
•Mydriasis produced is not accompanied by cycloplegia
•It is a fast acting mydriatic.
•One drop of 2.5% phenylephrine causing >5mmhg rise in IOP has
been used as a provoctive test for diagnosis of angle closure glaucoma.
•It is used in diagnosis of ptosis of Horner's Syndrome as it responds to
the instillation of 0.125 % phenylephrine drops.
•The diagnosis of Horner's syndrome can also be established as 1.0%
phenylephrine causes dilation of a horner’s pupil but not of a normal
pupil

Posterior Pole & Horner’s
Syndrome

Phenylephrine-Contra
Indications•Contraindications:
•Angle Closure glaucoma (ACG)
•Hypertensive patients: phenylephrine is a powerful
vasoconstrictor and is absorbed systemically when applied
topically to the eye.
•10% phenylephrine is contraindicated in infants.
•In patients receiving reserpine, guanethidine and tricyclic
antidepressants phenylephrine is contraindicated because of their
increased susceptibility to vasoconstriction action.
•In eyes where corneal epithelium is denuded it may cause corneal
clouding.
•Persons with a known hypersensitivity to any component.

Phenylephrine-Adverse Effects
•Ophthalmic:
•Mild Stinging (Pricking Pain (Needle)) on initial instillation
•Rebound(Move back or Return) conjunctival congestion on prolonged
use
•Rebound miosis may occur in some elderly patients
•Subsequent instillation my produce les mydriasis (elder patients)
•Systemic:(The Major difficulty in using this drug is the possibility of
inducing systemic HYPERTENSION, TACHYCARDIA, HEADACH
OR BROWACHE may occur.
•Episodes of myocardial infraction(little serious) and arrhythmias in
eolderly patients are reported.
•Stability:
•One other disadvantage is relatively short shelf life as once the bottle is
opened Phenylephrine rapidly oxidizes, which makes it less effective.

Phenylephrine - Dosage
•Dosage and Administration:
•Topically 1 or 2 Drops into the Conjunctiva of each eye for refraction, in
conjunction with some cycloplegic of choice.
•Maximum dilation with phenylephrine alone occurs within 15-60 mins
•The pupil size returns to normal within 4-6 hours.
•Initial instillation of a Topical Anaesthtic before phenylephrine prevent
st the Stinging caused by phenylephrine and enhances pupillary dilation.
•Premature infants:
•In premature infants for dilation, 2.5% phenylephrien is used in
conujunciton with 0.2% cyclopentolate or 0.5% tropicamide.

Mydriatics and Cycloplegics
Cycloplegics are drugs that cause Paralysis of ciliary muscles,
i.e., cause relaxation of accommodation.
•Various Types:
•Atropine Sulphate
•Homatropine Hydrobromide
•Cyclopentolate Hydrochloride
•Tropicamide

Atropine Sulphate
•Atropine Sulphate:
•It is a anti-cholinergic prepared as a sterile topical ophthalmic solution
and ointment supplied in three strengths
•0.5%, 1%, and 3%
•IM (Intramuscular ) injections are available as 0.3, 0.4, 0.6 mg/ml
preparations
•Mechanism of Action:
•Atropine sulphate is a naturally occurring that acts directly on the
muscarine receptors of structure innervated by the postganglionic
parasympathetic fibers.
•It does not reduce liberation(dismissal) of acetylcholine, but tissues are
rendered (Cause to become) sensitive to it.
•It is the competitive inhibitor of the muscarine action of acetylcholine
and is the strongest of the drug available for cycloplegic purposes
•It causes mydriasis and cycloplegic by paralyzing sphincter Pupillae and
ciliary muscle respectively.

Anti-Cholinergic Action of ATROPINE

Atropine-Indications
•Indications:
•It is used for mydriasis and cycloplegia(in young patients in which
accommodation is very active)
•Pupillary dilation in inflammatory conditions of the iris (to prevent pain,
release synechiae and give rest to inflamed tissue)
•In ciliary block glaucoma
•It is used to prevent undue vagal response in tensilon test.
•Amblyopia therapy (penalization)
•In cases of accommodative spasm
•Pre and post operatively in many intra-ocular surgeries.
•Contra indications:
•Primary glaucoma or a tendency towards glaucoma e.g. Narrow anterior
chamber angle.
•Hypersensitivity to any component of this preparation.

Atropine-Precautions &
Reactions•Precautions:
•Not use in Children- Due to Systemic absorption(Lacrymal Sac)
•Compress lacrimal Sac for One Minute-for Stop Systemic absroption
•LOCAL: Allergic(lids&Conjunctiva), Redness and Crusty flaking of the
eyelid margins, dryness and wrinkling of the skin around the eyelids and
injected bulbar conjunctiva with some watery discharge. Blurred vision
and photophobia are consequent to the cycloplegic and mydriatic effect
of atropine
•SYSTAMIC : Dryness of skin and mouth, tachyocardia, irritability or
delirium, flushing of face, skin rash, abdominal distension in infants and
hyperpyrexia may occur in children. Severe reaction are manifest by
hypotension with progressive respiratory depression. The elderly are
more susceptible to anti-cholinergic toxicity like cognitive impairment
and delirium.

Atropine-Dosage and
Administration
•Because of a long duration of its effect and delay in the
onset of action it is not routinely used for office
procedures.
CHILDREN: For refraction, administer 1% ointment
to each eye, thrice daily for three days prior to
examination.

HOMATROPINE HYDROBROMIDE
•Homatropine Hydrobromide:
•Homatropine 2% sterile ophthalmic solution was the first anit-
cholinergic to be developed specifically as an alternative to atropine.
•It is a synthetic anti-cholinergic agent that directly blocks the
muscarinic action of acetylcholine, causing mydriasis and cycloplegia.
•Its effect generally lasts longer than those of either cyclopentolate or
Tropicamide but it is not necessarily more effective.
•Homatropine is therefore not commonly used as diagnostic agent,
however its relatively long lasting effect makes it valuable in the
treatment of anterior ocular inflammations such as iritis.
•Indications and Usage:
•As a moderately long acting mydriatic and cycloplegic agent for
cycloplegic refraction and in the treatment of inflammatory condition of
the uveal tract.
•It is inferior to atropine for penalization therapy of amblyopia.

HOMATROPINE HYDROBROMIDE
•Contraindications:
•In Persons with a tendency of occludable angles.
•It should not be used in patients who have shown allergy to atropine.
Patient Warning:
 Patient should be advised not to drive or engage in other hazardous activities
while pupils are dilated.
 Caution also in pregnant and lactating mothers.
Adverse Reaction:
• similar to atropine but much less in frequency.
•Prolonged use may produce local irritation characterized by follicular
conjunctivitis, vascular congestion, edema, exudate and an eczematous
dermatitis.
•For refraction instill one or two drops topically in the eye(s).
•May be repeated in 5 to 10 minutes if necessary.

Cyclopentolate Hydrochloride
•Cyclopentolate Hydrochloride:
•Cyclopentolate 1% is an anti-cholinergic prepared as a sterile
ophthalmic solution.
•Also available as 0.5% and 2% solution.
•Indications:
•Cyclopentolate is an effective anti-muscarinic agent and the cycloplegic
of choice for children under age 12 and for youths between 12 and 20
when latent hyperopia or accommodative esotropia is suspected.
•Its cycloplegic efficacy is greater than homatropine.
•Also used for pre and post-operative states when mydriasis is required
and when a short acting mydriatic cycloplegic is needed in the therapy of
iridocyclitis.
•Unlike atropine and homatropine onset of maximum cycloplegia
approximates the onset of maximum mydriasis.
•It can also be used in patient with central lenticular changes, if they feel
better with mydriasis, till the patient is ready for surgery.

•Contraindications:
•Angle Closure glaucoma and in patients with hypersensitivity to the
drug.
•Cyclopentolate is also not recommended for children with emotional
problems since it can have marked central nervous system effects that
may be increase in susceptible youngsters.
•Adverse reaction:
•Local: increased intra ocular pressure, blurred vision, and photophobia
•Systemic: psychotic reactions, behavioral disturbances, seizures,
disorientation and cardio-respiratory collapse in children have been
reported.
•Dryness of the mouth , tachycardia, headache or allergic reaction may
occur.
•Because toxic reactions occur with multiple installations of 1% solution,
the smallest does should be used
•Management of over dosage in life threatening toxicity includes slow
injection of Physostigmine intravenously

Dosage & Administration
One drop followed by second drop in 5 Minutes or as
desired by the physician complete recovery usually
occurs in 24 hours.

Tropicamide
•Tropicamide:
•It is one of the most commonly used anti-cholinergic mydriatic because
of tis powerful mydriatic effects, rapid onnset of action and low
incidence of side effects.
•Ti is available as 0.5% or 1% eye drops
•Tropicamide acts by blocking muscarinic acetylcholine receptors.
•The stronger preparation (1%) also paralyses accommodation.
•The 0.5% strength may be useful in producing mydriasis with only
slight cycloplegia.
•Indications and usage:
•For mydriasis and cycloplegia, for diagnostic procedures and when a
short acting mydriatic is needed for some pre and post –operative stages.
•Unlike atropine, homatropine and cyclopentolate, pupillary dilation with
tropicamide is less dependent on iris pigmentation.
•For premature infants a combinations of 2.5%phynylephrine and 0.5%
tropicamide is recommended because the latter alone fails to dilate
adequately.

Tropicamide
•Contra indications:
•Contraindicated in angel closure glaucoma and in persons showing
hypersensitivity to any component of this preparation.
•Precautions:
•In the elderly and others where increased intra-ocular pressure may be
encountered, Mydriatics and Cycloplegics should be used with caution.
•This preparation may cause CNS disturbances that may be dangerous in
infants and children.
•Local: Stinging sensation
•Systemic: Rarely in children, confusion or hyperactivity may occur.
•Dosage and administration:
•One or two drops of 1% solution in each eye 2 to 3 times at 5 minutes
intervals or as directed by the physician.

Onset & Recovery of Cycloplegics

Miotics mydriatics cycloplegics

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