Medicines affecting the

afferent system
 Classification
Inhibitors
• Local anesthetics
• Astrigent drugs
• Demulcents
• Adsorbents
Stimulants
• Irritating drugs
Local anesthetics
• Local anesthetics reversibly block
impulse conduction along axons and
other excitable membranes that utilize
sodium channels as the primary means
of action potential generation.
• This action can be used clinically to
block pain sensation.
 Classification of local anesthetics

Duration of action:
• short acting (< 60 min) procaine
• medium acting ( 60-90 min ): lidocaine,
articaine, mepivacaine, prilocaine, trimecaine
• long acting(> 120 min): bupivacaine
 Classification of local anesthetics

Chemical structure
esters:
procaine, tetracaine, benzocaine
amides:
lidocaine, trimecaine, articaine, mepivacaine,
prilocaine, bupivacaine, ropivacaine, etidocaine
 Mechanism of Action

• The mechanism of local anesthetics connects with the ion channels,

nerve, and depolarization.
• Local anesthetics block the conduction in peripheral nerves that
inhibited the nerve to excited and created anesthesia.
• The anesthetic is a reversible reaction. It binds and activates the
sodium channels.
• The sodium influx through these channels and depolarizes the nerve
cell membranes. It also created high impulses along the way.
• As a result, the nerve loses depolarization and the capacity to create
the impulse, the patient loses sensation in the area supplied by the
nerve.
Mechanism of Action
 Types of local anesthetics

1.surface/topical anesthesia is often used for eye, ear,

nose, and throat procedures. Satisfactory anesthesia
requires an agent capable of rapid penetration of
the skin or mucosa. Tetracaine, because of its
excellent penetration .
2. Infiltration anesthesia: Local anesthetics is
injected in the vicinity of peripheral nerve endings
(such as area of the surgical incision).
3.conduction anesthesia Local anesthetics is injected
in the vicinity of major nerve trunks.
4 Spinalan (Subarachnoid) anesthesia :
Local anesthetics is instilled within the
subarachnoid spaces surrounding the
spinal cord.
5.Epidural anesthesiaLocal anesthetics is
instilled within the epidural spaces
surrounding the spinal cord.
• Local Anesthetics Cocaine is the first local
anesthetic (for ophthalmic use, 1884)
introduced into clinical practice. Its chronic
use was associated with psychological
dependence (addiction).
• Procaine was synthesized to improve upon
the clinical properties of cocaine (1905), and
became the dominant local anesthetic for ~
50 years.
• Lidocaine (1943) is the most widely used
local anesthetic.
 Toxicity of Local Anesthetics

Ultimately, local anesthetic agents are absorbed from

the site of administration. If blood levels rise too high,
effects on several organ system may be observed.
1.Hypersensitivity(allergic)
2. Central Nervous System: Central nervous system
effects at low doses include sleepiness, light- headedness,
visual and auditory disturbances, and restlessness. At
higher concentration, nystagmus muscular twitchingmay
occur. Finally overt tonic-clonic convulsions followed by
central nervous system depression and death may occur.
3. Cardiovascular System:
• Local anesthetics block cardiac sodium
channels and thus depress excitability and
conduction.
• At very high concentration, because they may
also block calcium channels, they depress the
strength of cardiac contraction and cause
arteriolar dilation. Both effects leads to
hypotension
 Demulcents
• Demulcent forms a soothing film over a
mucous membrane, relieving minor pain and
inflammation of the membrane;
• Demulsents are sometimes reffered to as
mucoprotective agents;
• Demulcents as pectin, glycerine, honey and
syrup are common ingredients in cough
mixtures
 Herbal demulcents
• Starch
• Flaxseed (Linum usitatissimum)
Demulcents have these general properties

• They reduce irritation down whole length

of the bowel.
• They reduce the sensitivity of the
digestive system to gastric acids.
• Help to ease the digestive muscle spasms
which cause colic.
Actions and uses of Demulcents:
• Protective action on mucous membranes and abraded skin. They
form a layer which covers the surface of the mucous membrane, thus
protecting it against irritant and noxious stimuli as mucin in case of
gastric ulcer
• Masking the bad taste of drugs through covering the taste buds of the
tongue and by adsorbing drug molecules thus preventing their
contact with the taste buds
• Delaying the absorption of drugs as inclusion of gelatin in the depot
form of heparin results in delayed absorption and prolonged duration
• Delaying the excretion of drugs as Gum administered with saline
delays its excretion
• Employed as emulsifying and suspending agents
 Astringents
The word "astringent" derives from
Latin adstringere, meaning "to bind
fast". •
Definition- Astringent is a drug that
reacts chemically with cellular proteins
producing limited coagulation which is
accompanied with shrinkage of body
tissues.
 CHARACTERISTICS
• Affect only the superficial layer. Reduce
cellular permeability.
• Make the surface mechanically stronger,
decrease exudation.
• Protect from external irritation.
• Possess local styptic and local antiseptic action.
• May interfere with the function of pain
receptors. The pain relieving action is mild.
 TYPES OF ASTRINGENTS
1. Organic astringents – tannic, gallic acid,
cortex of oak, leaves of chamomiles and sage.
2. Inorganic astringents – • Aluminium salts –
alum, aluminium chloride, aluminium acetate •
Zinc salts – zinc chloride, zinc sulfate • Ferric
chloride • Strontium chloride • Silver nitrate and
copper sulfate
 Uses of astringents:
• Cleaning the face and preventing Acne
Breakouts
• Stopping bleeding
• Relieving the discomfort and itching of insect
bites, minor abrasions and Athlete’s foot
• Haemorrhages
 Adsorbent
• It is the substance which adsorbs the other
substance at its surface.
Classification
• Activated carbon, also called activated
charcoal
• Talc
Classification
• Activated carbon, also
called activated charcoal
• Talc
 Mechanism of action
• Binding of the toxin to prevent stomach and
intestinal absorption. Binding is reversible so a
cathartic such as sorbitol may be added as
well.
• It interrupts the enterohepatic and
enterenteric circulation of some drugs, toxins
and their metabolates
 Indication for the use
• Activated carbon is used to treat poisonings
and overdoses following oral ingestion.
• Talc. It is native hydrous magnesium silicate,
which easily-used in talcum/face powders.
Entering raw surfaces, it can form granulomas-
should not be sprikled on wound or used
forbsurgical gloves.
 Irritants
• Irritants stimulate sensory nerve endings and
induce inflammation at the site of application.
• Depending on their nature, concentration and
sensitiveness of the site, they produce cooling
sensation or warmth, pricking and tingling,
hyperesthesia or numbness and local
vasodilatation.
 Classification
• Turpentine oil
• Menthol
• Mustard seeds
• Capsicum