Ocular hypotensive drugs
and
Antiglaucoma drugs
Ocular hypertension
Ocular hypertension is an eye pressure of
greater than 21 mm Hg.
An intraocular pressure of greater than 21 mm
Hg is measured in one or both eyes.
Normal eye pressure
Eye pressure is measured in millimeters of mercury
(mm Hg).
Normal eye pressure ranges from 12-22 mm Hg, and
eye pressure of greater than 22 mm Hg is considered
higher than normal.
When the IOP is higher than normal but the person
does not show signs of glaucoma, this is referred to
as ocular hypertension.
Glaucoma
A common eye condition in which the fluid
pressure inside the eye rises to a level higher
than healthy for that eye.
If untreated, it may damage the optic nerve,
causing the loss of vision or even blindness.
Symptoms and sign of glaucoma
Intense pain.
Redness of the eye.
Headache.
Tender eye area.
Seeing halos or 'rainbow-like' rings
around lights.
Loss of vision in one or both eyes that
Progresses very quickly.
Increase intraocular pressuse
Glaucoma is characterized by progressive damage
to the optic nerves
Ocular hypotensive drugs
Ocular hypotensive drugs are used to reduced the
intraocular pressure.
Ocular hypotensive drugs classification
A..Prostaglandins analogues
Latanoprost
Travoprost
Bimatoprost
B..Beta-Adrenergic antagonist( b-blockers)
Timolol
Levobunolol
Betaxolol
Carteolol
Ocular hypotensive drugs classification
C.. Adrenergic agonist
Apraclonidine
Brimonidine
D..Carbonic Anhydrase inhibitor
Acetazolamide
Methazolamide
Dorzolamide
Brinzolamide
E..Cholinergic agonist(Miotics)
Pilocarpine
1..Prostaglandins analogues:
Prostaglandins analogues are first line treatment for
most patient with ocular hypertension and open-angle
glaucoma.
Latanoprost the first commercially successful
prostaglandins for clinical used in treatment of
glaucoma.
Latanoprost
MOA: (Mechanism of action)
It is a prostaglandin (PG)F2α analog.
It is believed to reduced the intraocular
pressure by increasing outflow of aqueous
humor.
Uses/Indication:
Used in treatment of open-angle glaucoma or ocular
hypertension in patient who are intolerant of other
intraocular pressure lowering medication.
Lanatoprost may be used alone or in combination
with other antiglaucoma agents.
Open-angle glaucoma, also called chronic glaucoma
Closed angle glaucoma, also called acute glaucoma,
Adverse effect
Blurred vision
Ocular burning
Ocular pain
Dry eyes
Hyperlacrimation
Photophobia
Contraindication
Hypersensitive to drug, if inflammation occur.
2..β-blockers/β-adrenergic antagonist
Timolol:
Timolol is a beta-adrenergic blocking agent.
Non-selective, antagonize beta-1 and beta-2.
Like other beta-adrenergic blocking agents, it
mainly blocks the action of the sympathetic
(adrenergic) nervous system.
Mechanism of action
Timolol causes a reduction of the pressure within the eye
(intraocular pressure). This effect is may result from a
reduction in production of the liquid (aqueous humor)
within the eye.
The precise mechanism of this effect is not known.
The reduction in intraocular pressure reduces the risk of
damage to the optic nerve and loss of vision in patients
with glaucoma.
Indication/use:
Used for lowering intraocular pressure
for treatment of glaucoma, acute-angle glaucoma.
Contraindication:
Hypersensitive to drug or class
Asthma/bronchial problem
Bradycardia
Severe heart block
Severe COPD
Adverse effect
Bradycardia
Heart block
Bronchospasm
3..Adrenergic Agonist
Since early 1920s Epinephrine used as to reduced
IOP.(non-selective adrenergic agonist)
so currently used α2-receptor agonist are ,adrenergic
agonist of choice for glaucoma.
Apraclonidine
Brimonidine
Apraclonidine
Mechanism of action:
Selective α-2 adrenoceptor agonist , derivative of
antihypertensive agent clonidine.
Apraclonodine lowers the intraocular pressure by
decreasing aqueous production.
4..Carbonic Anhydrase inhibitor
Acetazolamide
Brinzolamide
Dorzolamide
Methoxazole
Mechanism of action
It reversibly blocks the enzyme carbonic anhydrase in the
ciliary body and thus suppresses aqueous humor
production.
The Aquous fluid rich in sodium and bicarbonate ions is
hyperosmotic as compared to plasma.
Water is attracted to the posterior chamber as a result of
osmosis and the high concentration of bicarbonate ions is
diluted.
Uses /Indication:
1..Used in treatment of all type of glaucoma.
2..Used in treatment of elevated IOP, Often
reserved for short-term IOP reduction only.
3..produce an additional decrease in IOP ,when
added to drug regimen ,including, Miotics, B-
blockers and prostaglandins.
Contraindication:
Hypersensivity to drug.
Pregnancy
Severe obstructive pulmonary disease
Side effect of Acetazolamide:
Transient myopia
Dermatitis
Hypokalemia
Fatigue
Weight loss
5..Cholinergic Agonist(Miotics)
Classification of cholinergic agonist
Direct acting:
Acetylcholine
Methacholine
Pilocarpine
Carbachol
Indirect acting
(Cholinesterase inhibitor)
(Reversible) Irreversible
Physostigmine Ecothiophate
Neostigmine
Edrophonium
Demacarium
Mechanism of Action:
Produce biological response similar to those of
acetylcholine. these drugs also known as
Parasympathomimetics or cholinomimetics.
In clinical practice referred as Miotics.
Direct Acting drugs:
Activates cholinergic receptors directly at
neuroeffector junctions of iris sphincter muscle
and ciliary body.
Indirect acting drugs:
Exert their cholinergic effect by inhibiting
cholinesterase and increase amount available at
cholinergic receptors.
Pilocarpine
An alkaloid of natural plant origin. Pilocarpine is a
direct acting cholinergic agonist.
Mechanism of action
Pilocarpine is a direct acting cholinergic
parasympathomimetic agent which acts through
direct stimulation of muscarinic receptors and
smooth muscle such as the iris and secretory
glands.
Pilocarpine contracts the ciliary muscle, causing
opening of the trabecular meshwork spaces to
facilitate outflow of aqueous humor.
Uses/indication
Most useful miotic for management of acute angle
closure glaucoma and many secondary glaucomas.
Also used along with other agents.
At high IOP of 60mmHg, topical beta-
blockers,apraclonidine or systemic agents are indicated
initially to bring pressuse below 50mmHg.
Contraindication:
Presence of cataract
Patients younger than 40 year of age
Asthma or history of asthma
6..Hyperosmotic agents
These agents act by enhancing the osmotic pres-
sure of plasma with respect to intraocular
structures thereby setting an osmotic gradient.
Consequently the fluid moves from the eye to
hyperosmotic plasma of ocular blood vessels,
thereby reducing the vitreous volume which is
responsible for lowering of IOP.
Hyperosmotic agents classification
Include
oral glycerin and isosorbide orally,
mannitol and urea intravenously.
Uses and indication
The use of these drugs is currently limited to short
term emergency situations
such as acute angle closure glaucoma or pre-
operative control of raised IOP.
Hyperosmotic agents
These drugs are usually for people with a severely high
IOP that must be reduced immediately before
permanent, irreversible damage occurs to the optic nerve.
Hyperosmotic agents reduce IOP by lowering fluid
volume in the eye.
Side effects
The side effects of these drugs include
nausea,
vomiting,
diuresis,
headache,
diarrhea,
chills and fever.

Ocular hypotensive drugs

  • 1.
  • 3.
    Ocular hypertension Ocular hypertensionis an eye pressure of greater than 21 mm Hg. An intraocular pressure of greater than 21 mm Hg is measured in one or both eyes.
  • 4.
    Normal eye pressure Eyepressure is measured in millimeters of mercury (mm Hg). Normal eye pressure ranges from 12-22 mm Hg, and eye pressure of greater than 22 mm Hg is considered higher than normal. When the IOP is higher than normal but the person does not show signs of glaucoma, this is referred to as ocular hypertension.
  • 5.
    Glaucoma A common eyecondition in which the fluid pressure inside the eye rises to a level higher than healthy for that eye. If untreated, it may damage the optic nerve, causing the loss of vision or even blindness.
  • 7.
    Symptoms and signof glaucoma Intense pain. Redness of the eye. Headache. Tender eye area. Seeing halos or 'rainbow-like' rings around lights. Loss of vision in one or both eyes that Progresses very quickly. Increase intraocular pressuse Glaucoma is characterized by progressive damage to the optic nerves
  • 8.
    Ocular hypotensive drugs Ocularhypotensive drugs are used to reduced the intraocular pressure.
  • 11.
    Ocular hypotensive drugsclassification A..Prostaglandins analogues Latanoprost Travoprost Bimatoprost B..Beta-Adrenergic antagonist( b-blockers) Timolol Levobunolol Betaxolol Carteolol
  • 12.
    Ocular hypotensive drugsclassification C.. Adrenergic agonist Apraclonidine Brimonidine D..Carbonic Anhydrase inhibitor Acetazolamide Methazolamide Dorzolamide Brinzolamide E..Cholinergic agonist(Miotics) Pilocarpine
  • 13.
    1..Prostaglandins analogues: Prostaglandins analoguesare first line treatment for most patient with ocular hypertension and open-angle glaucoma. Latanoprost the first commercially successful prostaglandins for clinical used in treatment of glaucoma.
  • 14.
    Latanoprost MOA: (Mechanism ofaction) It is a prostaglandin (PG)F2α analog. It is believed to reduced the intraocular pressure by increasing outflow of aqueous humor.
  • 15.
    Uses/Indication: Used in treatmentof open-angle glaucoma or ocular hypertension in patient who are intolerant of other intraocular pressure lowering medication. Lanatoprost may be used alone or in combination with other antiglaucoma agents.
  • 16.
    Open-angle glaucoma, alsocalled chronic glaucoma Closed angle glaucoma, also called acute glaucoma,
  • 17.
    Adverse effect Blurred vision Ocularburning Ocular pain Dry eyes Hyperlacrimation Photophobia Contraindication Hypersensitive to drug, if inflammation occur.
  • 18.
    2..β-blockers/β-adrenergic antagonist Timolol: Timolol isa beta-adrenergic blocking agent. Non-selective, antagonize beta-1 and beta-2. Like other beta-adrenergic blocking agents, it mainly blocks the action of the sympathetic (adrenergic) nervous system.
  • 19.
    Mechanism of action Timololcauses a reduction of the pressure within the eye (intraocular pressure). This effect is may result from a reduction in production of the liquid (aqueous humor) within the eye. The precise mechanism of this effect is not known. The reduction in intraocular pressure reduces the risk of damage to the optic nerve and loss of vision in patients with glaucoma.
  • 20.
    Indication/use: Used for loweringintraocular pressure for treatment of glaucoma, acute-angle glaucoma.
  • 21.
    Contraindication: Hypersensitive to drugor class Asthma/bronchial problem Bradycardia Severe heart block Severe COPD Adverse effect Bradycardia Heart block Bronchospasm
  • 22.
    3..Adrenergic Agonist Since early1920s Epinephrine used as to reduced IOP.(non-selective adrenergic agonist) so currently used α2-receptor agonist are ,adrenergic agonist of choice for glaucoma. Apraclonidine Brimonidine
  • 23.
    Apraclonidine Mechanism of action: Selectiveα-2 adrenoceptor agonist , derivative of antihypertensive agent clonidine. Apraclonodine lowers the intraocular pressure by decreasing aqueous production.
  • 24.
  • 25.
    Mechanism of action Itreversibly blocks the enzyme carbonic anhydrase in the ciliary body and thus suppresses aqueous humor production. The Aquous fluid rich in sodium and bicarbonate ions is hyperosmotic as compared to plasma. Water is attracted to the posterior chamber as a result of osmosis and the high concentration of bicarbonate ions is diluted.
  • 26.
    Uses /Indication: 1..Used intreatment of all type of glaucoma. 2..Used in treatment of elevated IOP, Often reserved for short-term IOP reduction only. 3..produce an additional decrease in IOP ,when added to drug regimen ,including, Miotics, B- blockers and prostaglandins.
  • 27.
  • 28.
    Side effect ofAcetazolamide: Transient myopia Dermatitis Hypokalemia Fatigue Weight loss
  • 29.
    5..Cholinergic Agonist(Miotics) Classification ofcholinergic agonist Direct acting: Acetylcholine Methacholine Pilocarpine Carbachol
  • 30.
    Indirect acting (Cholinesterase inhibitor) (Reversible)Irreversible Physostigmine Ecothiophate Neostigmine Edrophonium Demacarium
  • 31.
    Mechanism of Action: Producebiological response similar to those of acetylcholine. these drugs also known as Parasympathomimetics or cholinomimetics. In clinical practice referred as Miotics.
  • 32.
    Direct Acting drugs: Activatescholinergic receptors directly at neuroeffector junctions of iris sphincter muscle and ciliary body. Indirect acting drugs: Exert their cholinergic effect by inhibiting cholinesterase and increase amount available at cholinergic receptors.
  • 33.
    Pilocarpine An alkaloid ofnatural plant origin. Pilocarpine is a direct acting cholinergic agonist.
  • 34.
    Mechanism of action Pilocarpineis a direct acting cholinergic parasympathomimetic agent which acts through direct stimulation of muscarinic receptors and smooth muscle such as the iris and secretory glands. Pilocarpine contracts the ciliary muscle, causing opening of the trabecular meshwork spaces to facilitate outflow of aqueous humor.
  • 36.
    Uses/indication Most useful mioticfor management of acute angle closure glaucoma and many secondary glaucomas. Also used along with other agents. At high IOP of 60mmHg, topical beta- blockers,apraclonidine or systemic agents are indicated initially to bring pressuse below 50mmHg.
  • 37.
    Contraindication: Presence of cataract Patientsyounger than 40 year of age Asthma or history of asthma
  • 38.
    6..Hyperosmotic agents These agentsact by enhancing the osmotic pres- sure of plasma with respect to intraocular structures thereby setting an osmotic gradient. Consequently the fluid moves from the eye to hyperosmotic plasma of ocular blood vessels, thereby reducing the vitreous volume which is responsible for lowering of IOP.
  • 39.
    Hyperosmotic agents classification Include oralglycerin and isosorbide orally, mannitol and urea intravenously.
  • 40.
    Uses and indication Theuse of these drugs is currently limited to short term emergency situations such as acute angle closure glaucoma or pre- operative control of raised IOP.
  • 41.
    Hyperosmotic agents These drugsare usually for people with a severely high IOP that must be reduced immediately before permanent, irreversible damage occurs to the optic nerve. Hyperosmotic agents reduce IOP by lowering fluid volume in the eye.
  • 42.
    Side effects The sideeffects of these drugs include nausea, vomiting, diuresis, headache, diarrhea, chills and fever.