Orabloc is indicated in adults, adolescents and children of 4 years and older for local
anaesthesia (infiltration and nerve-block anaesthesia) in dentistry:
- mucosal and bone surgery requiring stronger ischaemia,
- dental pulp surgery (amputation and extirpation),
- extraction of fractured teeth (osteotomy),
- protracted surgical interventions,
- percutaneous osteosynthesis,
- cystectomy,
- mucogingival interventions,
- apicoectomy

Posology
For uncomplicated forceps extraction of the upper teeth where no inflammation is
present, a vestibular injection of 1.8 ml per tooth is usually sufficient. In isolated
cases, an additional vestibular injection of 1-1.8 ml may be necessary to achieve
complete anaesthesia. Injection via the painful palatine route is normally not
necessary.
Where the palate requires incision or suture, a palatine depot of about 0.1 ml per
puncture is sufficient. Where multiple extractions of adjacent teeth are necessary, it is
possible in most cases to reduce the number of vestibular injections required.
In uncomplicated forceps extraction of lower premolars where no inflammation is
present, injection of 1.8 ml per tooth is usually sufficient. However, if the anaesthesia
is incomplete, an additional vestibular injection of 1-1.8 ml is recommended.
Conventional mandibular anaesthesia is indicated only where the above mentioned
procedure does not result in a complete anaesthesia.
For surgical operations, it is recommended that the dose of Orabloc be adjusted
individually based on the operation’s severity and duration.
Over the course of treatment, adults may be given up to 7 mg articaine per kg body
weight. Using the aspiration technique, doses of up to 500 mg (equivalent to 12.5 ml
of solution for injection) were well tolerated.
Elderly patients and patients with severe hepatic and renal dysfunction
Increased plasma articaine levels may occur in elderly patients and in patients with
severe hepatic and renal dysfunction. In such patients, particular care should be taken
to use the minimum dose needed to achieve required anaesthesia.
Paediatric population
When using Orabloc in children and adolescents, the minimum volume necessary to
achieve adequate anaesthesia should be used; the injection amount should be
individually tailored to the age and weight of the child and adolescent.
A maximum dose of 5 mg articaine per kg of body weight should not be exceeded.
This product has not been studied in children less than 1 year old.
Method of administration
For use in dental anaesthesia only.
Before injection, aspiration is always recommended to avoid intravascular injection.
Aspiration should be performed in two stages, i.e. needle rotation by 90° or even
better by 180°.
Major systemic reactions as a result of accidental intravascular injection can be
avoided in most cases by an injection technique – after aspiration, slow injection of
0.1–0.2 ml and slow application of the rest – not earlier than 20–30 seconds later.
To avoid risk of infection (e.g. hepatitis transmission), syringe and needles used to
draw up the solution must always be fresh and sterile.
For single use. Any unused solution should be discarded.
This medicinal product should not be used if cloudy or discoloured.

Hypersensitivity to the active substances or to any of the excipients listed in section 6.1. On account of the effect of the articaine content, Orabloc must not be used in: - hypersensitivity to other local anaesthetics of the amide type, - severe cardiac impulse formation and conduction disturbances (e.g. 2nd or 3rd degree AV block, marked bradycardia), - acute decompensated heart failure (acute congestive heart failure), - severe hypotension, - children under 4 years of age. On account of the effect of the adrenaline (epinephrine) content, Orabloc must not be used in: - anaesthesia of the terminal nerve branches, - patients with narrow-angle glaucoma, - patients with hyperthyroidism, - patients with paroxysmal tachycardia or absolute arrhythmias with rapid heart rate, - patients with recent (3 to 6 months) myocardial infarction, - patients with recent (3 months) coronary artery bypass surgery, - patients taking non-cardioselective beta-blockers (e.g. propranolol), (risk of hypertensive crisis or severe bradycardia), - patients with phaeochromocytoma, - patients with severe hypertension, - concomitant treatment with tricyclic antidepressants or MAO inhibitors, as these active substances can intensify the cardiovascular effects of adrenaline (epinephrine). This can occur up to 14 days after MAO inhibitor treatment has ended. Intravenous use is contraindicated. Orabloc must not be used in persons with bronchial asthma with hypersensitivity to sulphites. In such individuals, Orabloc may precipitate acute allergic reactions with anaphylactic symptoms, such as bronchospasm.

In patients with cholinesterase deficiency, Orabloc must only be given in the presence
of compelling indications, since its action is likely to be prolonged and may
sometimes be too strong.
Orabloc must be used with particular caution in cases of:
- blood coagulation disturbances,
- severe renal or hepatic dysfunction,
- concomitant treatment with halogenated inhalation anaesthetics (see section 4.5),
- history of epilepsy (see section 4.8),
and use of Orabloc 1:200,000 solution for injection
over Orabloc 1:100,000
solution for injection should be considered on account of its lower adrenaline
(epinephrine) content of 0.005 mg/ml in patients with:
- cardiovascular diseases (e.g. heart failure, coronary heart disease, angina
pectoris, history of myocardial infarction, cardiac arrhythmia, hypertension),
- arteriosclerosis,
- cerebral circulation disturbances, history of strokes,
- chronic bronchitis, pulmonary emphysema,
- diabetes mellitus,
- severe anxiety.
Injection into an inflamed (infected) area is discouraged (increased uptake of Orabloc
with reduced efficacy).
Before using this product it is necessary to ask the patient questions on medical
history, concomitant treatment and to keep verbal contact with patient, and to practice
an injection test with 5 or 10% of the dose in case of risk of allergy.
To avoid occurrence of adverse effects the following must be taken into account:
- choose the lowest possible dose,
- before injection, aspiration in two stages (to avoid inadvertent intravascular
injection).
Equipment and drugs necessary for monitoring and emergency resuscitation should
be immediately available (Oxygen, anticonvulsive drugs as benzodiazepines or
barbiturates, muscle relaxants, atropin and vasopressin or epinephrine (adrenalin) in
case of severe allergic or anaphylactic reactions).
It is recommended that the patient refrain from eating until the anaesthesia has worn
off.
Paediatric population
Carers of young children should be warned of the risk of accidental soft tissue injury
due to self-biting, due to prolonged soft tissue numbness.
This medicinal product contains metabisulphite (E223) which may rarely cause
severe hypersensitivity reactions and bronchospasm.
This medicinal product contains less than 1 mmol sodium (23 mg) per dose, i.e.
essentially ‘sodium-free’.

Combinations of different anaesthetics cause additive effects on cardiovascular
system and CNS.
The blood-pressure-increasing effects of sympathomimetic-type vasoconstrictors
(such as adrenaline) may be intensified by tricyclic antidepressants or MAO
inhibitors and these are therefore contraindicated (see section 4.3).
For concomitant use of non cardioselective beta-blockers, see section 4.3.
Adrenaline (epinephrine) may inhibit the release of insulin in the pancreas, thereby
attenuating the effect of oral antidiabetics.
Certain inhalation anaesthetics, such as halothane, may increase myocardial
sensitivity to catecholamines, and may therefore precipitate arrhythmias following
administration of Orabloc.
Phenothiazines can influence the blood-pressure-increasing effects of epinephrine.
Therefore concomitant treatment should be avoided. If concomitant treatment is
necessary patients should be monitored carefully.
It should be remembered that, in patients receiving anticoagulation treatment (e.g.
heparin or acetylsalicylic acid), inadvertent vascular puncture during local anaesthesia
may lead to serious bleeding, and that the tendency to bleed is generally increased in
such patients.

Pregnancy
There is no experience of the use of articaine in pregnant women, except during
childbirth. Animal studies do not indicate that articaine has direct or indirect harmful
effects on pregnancy, embryonal/foetal development, birth or postnatal development.
Animal studies have shown that adrenaline (epinephrine) is toxic to reproduction at
doses higher than maximal recommended dose (see section 5.3).
Adrenaline (epinephrine) and articaine cross the placental barrier, although articaine
does so to a lesser extent than other local anaesthetics. Serum concentrations of
articaine measured in newborn infants were approx. 30% of maternal levels. In the
event of inadvertent intravascular administration in the mother, adrenaline
(epinephrine) can reduce uterine perfusion. During pregnancy, Orabloc should only
be used after a careful analysis of the benefit-to-risk ratio has been made.
On account of its lower adrenaline (epinephrine) content, use of Orabloc 1:200,000
solution for injection over Orabloc 1:100,000
solution for injection should be preferred.
Breastfeeding
As a result of the rapid drop in serum levels and rapid elimination, clinically relevant
quantities of articaine are not found in breast milk. Adrenaline (epinephrine) passes
into breast milk but also has a short half-life.
It is not usually necessary to suspend breast-feeding for short-term use.
Fertility
Animal studies with articaine 40 mg/ml + adrenaline (epinephrine) 0.01 mg/ml have
not shown effects on fertility (see section 5.3). At therapeutic doses, adverse effects
on human fertility are not expected.

After application of Orabloc the dentist must decide when a patient is capable again
of operating a vehicle or machinery.
Apprehension and operation related stress may affect performance capabilities;
although, in relevant tests, local anaesthesia with articaine caused no discernible
impairment in normal driving ability.

The following categories are used for classifying the frequency of undesirable effects:
Very common (≥1/10)
Common (≥1/100 to <1/10)
Uncommon (≥1/1.000 to <1/100)
Rare (≥1/10.000 to <1/1.000)
Very rare (<1/10.000)
Not known (cannot be estimated from the available data)
Immune system disorders
Not known: Allergic or allergy-like hypersensitivity type reactions. These may
manifest themselves as oedematous swelling and/or inflammation at the injection site
or manifestations appearing independently of the site may include skin reddening,
itching, conjunctivitis, rhinitis, facial swelling (angioedema) with swelling of the
upper and/or lower lip and/or cheeks, glottal oedema with globus pharyngis and
difficulty in swallowing, urticaria and difficulty in breathing which may progress to
anaphylactic shock.
Nervous system disorders
Common: paresthesia, hypoesthesia; headaches, due presumably to the adrenaline
component.
Uncommon: dizziness
Not known:
- Dose-related (particularly at excessively high dosages or after inadvertent
intravascular injection), central nervous system reactions may occur: agitation,
nervousness, stupor sometimes progressing to loss of consciousness, coma,
respiratory disorders sometimes progressing to respiratory arrest, muscular tremor
and muscular twitching sometimes progressing to generalised convulsions.
- Nerve lesions (e.g. facial nerve paresis) and reduced gustatory sensitivity in the
orofacial regionare not side effects specific to articaine. However, such reactions are
theoretically possible with any dental intervention, due to anatomical conditions in
the injection area or incorrect injection techniques.
Eye disorders
Not known: Temporary visual disturbances (blurred vision, blindness, double vision)
occurring during or shortly after injection of local anaesthetics in the area of the head.
Cardiac disorders
Uncommon: tachycardia
Not known: cardiac arrhythmias, rise in blood pressure, hypotension, bradycardia,
cardiac failure and shock (possibly life-threatening).
Respiratory, thoracic and mediastinal disorders
Not know: respiratory dysfunction (tachypnea, bradypnea) that may lead to apnea
Gastrointestinal disorders
Common: Nausea, vomiting.
General disorders and administration site conditions
Not known: inadvertent intravascular injection may lead to the development of
ischaemic zones in the injection site, sometimes progressing to tissue necrosis (see
also section 4.2).
On account of its sodium metabisulphite content, the product can precipitate
hypersensitivity reactions, particularly in patients with bronchial asthma. Such
reactions may manifest in vomiting, diarrhoea, wheezing, acute asthma attacks,
impaired consciousness or shock.
Paediatric population:
In published studies, the safety profile was similar in children and adolescents from 4
to 18 year old compared to adults. However, accidental soft tissue injury was
observed more frequently (in up to 16% of children), especially in 3 to 7 year old
children, due to the prolonged soft tissue anaesthesia. In a retrospective study of 211
children aged 1 to 4 years of age, dental treatment was carried out using up to 4.2 ml
of 4% articaine + 0.005 mg/ml or 0.01 mg/ml adrenaline (epinephrine), with no
reported side effects.
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is
important. It allows continued monitoring of the benefit/risk balance of the medicinal
product. Healthcare professionals are asked to report any suspected adverse reactions
viathe Yellow Card Scheme
Website: www.mhra.gov.uk/yellowcard or search for MHRA Yellow Card in the Google Play or Apple App Store.

a) Symptoms of over dosage
CNS stimulation: restlessness, anxiety, confusion, hyperpnoea, tachycardia, rise in
blood pressure with facial reddening, nausea, vomiting, tremor, twitching, tonicclonic
seizures.
CNS depression: dizziness, impairment of hearing, loss of ability to speak, loss of
consciousness, muscle atony, vasomotor paralysis (weakness, pallor), dyspnoea,
death due to respiratory paralysis.
Cardiovascular depression: bradycardia, arrhythmia, ventricular fibrillation, fall in
blood pressure, cyanosis, cardiac arrest.
b) Emergency measures and antidotes
At the first signs of side effects or intoxication, e.g. dizziness, motor restlessness, or
stupor, the injection should be stopped and the patient placed in a horizontal position.
The patient’s airway should be kept clear and pulse and blood pressure monitored.
It is recommended, including when the symptoms of intoxication seem not to be
severe, to insert an I.V. catheter, for immediate intravenous injections when
necessary.
In respiratory disorders, depending on their severity, the administration of oxygen, as
well as – where necessary – that of artificial respiration are recommended, as is where
necessary, the performance of endotracheal intubation and controlled ventilation.
Muscular twitching or generalised convulsions may be removed by intravenous
injection of a short acting antispasmodic (e.g. suxamethonium chloride, diazepam).
Artificial respiration (oxygen) is also recommended.
A fall in blood pressure, tachycardia, or bradycardia may be corrected simply by
placing the patient in a horizontal or slightly ‘head-down’ position.
In severe circulatory disturbances and shock – regardless of cause – the following
emergency measures should be immediately implemented after stopping the injection:
- place the patient in a horizontal or ‘head-down’ position and keep the patient’s
airways clear (oxygen insufflation),
- set up an intravenous infusion (balanced electrolyte solution),
- intravenous administration of a glucocorticoid (e.g. 250-1000 mg prednisolone
or the equivalent amount of a derivative, e.g. methylprednisolone),
- volume substitution (additionally, if necessary, plasma expander, human
albumin).
If circulatory collapse appears imminent and bradycardia worsens, intravenous
adrenaline (epinephrine) should be given immediately. After diluting 1 ml of a
commercial 1:1,000 adrenaline (epinephrine) solution to 10 ml (a 1:10,000 adrenaline
(epinephrine) solution can be used instead), 0.25 - 1 ml of the solution (= 0.025 - 0.1
mg adrenaline (epinephrine)) is injected slowly with monitoring of pulse and blood
pressure (caution: cardiac arrhythmias). Do not exceed 1 ml (0.1 mg adrenaline
(epinephrine)) per single intravenous injection. Where additional amounts of
adrenaline are required, recommendation is given to administering these together with
the infusion solution (adjust drip rate according to pulse rate and blood pressure).
Severe tachycardia and tachyarrhythmias may be treated with anti-arrhythmic drugs,
but not with noncardioselective beta-blockers, e.g. propranolol (see section 4.3). In
such cases, oxygen must be given and circulation monitored.
Increase of blood pressure in hypertensive patients must be treated with peripheral
vasodilators, if necessary.

Pharmacotherapeutic group: Anaesthetics, local; Amides.
ATC code: N01BB58
Orabloc is an acid amide-type local anaesthetic used for terminal and nerve-block
anaesthesia in dentistry. It is fast-acting (latency time 1-3 min) with a potent analgesic
effect and good tissue tolerability.
The duration of effective anaesthesia is about 45 min for Orabloc 0.005 mg/ml and
about 75 min for Orabloc 0.01 mg/ml.
The mechanism of action of articaine is assumed to be based on inhibition of
conduction in nerve fibres, due to blockade of voltage-dependent Na+ channels in the
cell membrane.
Its extremely low adrenaline (epinephrine) concentration and high intensity of action
make Orabloc 0.005 mg/ml suitable for use in patients with cardiovascular diseases.
Paediatric population
In children 3.5 to 16 years old, clinical studies including up to 210 patients, have
shown that 4% articaine + 0.005 mg/ml adrenaline (epinephrine) at doses up to 5
mg/kg and 4% articaine + 0.010 mg/ml adrenaline (epinephrine) at doses up to 7
mg/kg provided successful local anaesthesia , if given by (mandibular) infiltration or
(maxillary) nerve block. The anaesthesia duration was similar for all age groups and
depended on the volume administered.

In serum, articaine is bound to plasma-proteins at 95%. The elimination half-life after
intraoral submucosal injection is 25.3 ± 3.3 min. 10% of articaine is metabolised in
the liver, mainly by plasma and tissue esterases. Articaine is subsequently excreted
via the renal route, mainly as articainic acid.
In children, overall exposure after vestibular infiltration is similar to those in adults,
but maximum serum concentration is reached faster.

Preclinical data reveal no special hazard for humans at therapeutic doses, based on
conventional studies of safety pharmacology, chronic toxicity, reproductive toxicity
and genotoxicity. At supratherapeutic doses, articaine has cardiodepressant properties
and can exert vasodilatory effects.
Adrenaline (epinephrine) exhibits sympathomimetic effects.
In embryotoxicity studies with articaine, no increase in the foetal mortality rate or
malformations were observed at daily i.v. doses of up to 20 mg/kg (rat) and 12.5
mg/kg (rabbit). Adrenaline (epinephrine) showed reproductive toxicity in animals at
doses ranging from 0.1 to 5 mg/kg (several folds the maximal dose of adrenaline
(epinephrine) when using Orabloc) with evidence of congenital malformations and
impaired uteroplacental perfusion.
In embryofoetotoxicity studies with articaine and adrenaline (epinephrine), no
increase in malformations were observed at daily s.c. doses of articaine up to 80
mg/kg (rat) and 40 mg/kg (rabbit).
In a fertility and early embryonic development study in rats no adverse effects on
male or female fertility were noted at doses causing parental toxicity

Sodium chloride
Sodium metabisulfite (E223)
Hydrochloric acid 2% (for pH adjustment)
Water for injection

Not applicable

2 years

Do not store above 25°C. Store in the original package in order to protect from light.

Clear glass cartridges (Type I) closed at one end with a bromobutylic rubber plunger
and at the other with an aluminium cap and rubber seal.
The cartidge is available in different packages:
The cartridges are packaged in PVC blisters (10 cartridges/blister); the blisters are
packaged in a cardboard box containing 5 x 10 or 10 x 10 cartridges.
Each cartridge is assembled in a plastic injector; each injector containing a cartridge
is placed in a sealed blister; the injectors are packaged in a cardboard box together
with an Instructions for use of the injector: 50 or 100 units per commercial pack.
Not all pack sizes may be marketed.

As for any cartridge, the rubber seal (diaphragm) will be disinfected just before use
with either pharmaceutical grade ethyl alcohol (70%) or pharmaceutical grade
Isopropyl alcohol (90%).
The cartridges must not be immersed in the above solutions.
Do not mix the injectable solution with other products in the same syringe.
Any unused solution or waste material should be disposed of in accordance with local
requirements.