The powerful painkiller tramadol will be banned in-competition in cycling from March this year.
Cycling's world governing body, the UCI, has announced its own ban despite the drug not being included on the World Anti-Doping Agency (Wada) prohibited list.
Penalties for a positive test range from disqualification from the event to a nine-month ban for a third offence.
Tramadol was detected in 4.4% of all samples taken in cycling in 2017.
The UCI said the aim of the ban is "preserving the rider's health and safety" because of the side-effects of tramadol.
Possible side-effects include nausea and dizziness, while tramadol is also addictive and there are concerns it has caused crashes by making riders drowsy.
Wada's 2017 monitoring report showed that 68% of all urine samples containing tramadol taken from 35 Olympic sports were from cyclists.
Under the new ban, a rider testing positive for tramadol for the first time will be disqualified from the event they are tested at and fined 5,000 Swiss francs (£3,925).
A second offence will also result in disqualification and a five-month suspension, which increases to nine months for a third positive test.
Teams may also be punished, with any UCI-registered outfit facing a fine of 10,000 Swiss francs (£7,850) if two of their riders test positive in the same 12-month period.
A further offence within the same 12 months will see the team suspended for between one and 12 months, to be decided by the UCI disciplinary commission.
The UCI and the UK and US Anti-Doping Agencies have called on Wada to add tramadol to the banned list.
However, Wada said last year it is not yet convinced tramadol is performance-enhancing but could ban it if ongoing studies conclude it is.
British cyclist Josh Edmondson told BBC Sport in 2017 that he had severe depression after independently using tramadol while at Team Sky, after former rider Michael Barry had said he used the drug at the British outfit.
Team Sky said its policy is that none of its cyclists should ride while using tramadol and that it does not give the drug to riders while racing or training.
In 2016, former Team Sky rider Jonathan Tiernan-Locke told BBC Sport said he had been offered tramadol at the 2012 World Championships in the Netherlands when riding for Great Britain.
British Cycling said the doctor concerned - former chief medic Richard Freeman - denied Tiernan-Locke's claim.